Category: 18621-18-6

In 2012,Dillon, Barry R.; Roberts, Dannielle F.; Entwistle, David A.; Glossop, Paul A.; Knight, Craig J.; Laity, Daniel A.; James, Kim; Praquin, Celine F.; Strang, Ross S.; Watson, Christine A. L. published 《Development of a scaleable synthesis of a geminal dimethyl tertiary amine as an inhaled muscarinic antagonist for the treatment of COPD》.Organic Process Research & Development published the findings.Related Products of 18621-18-6 The information in the text is summarized as follows:

An efficient and scaleable process for the synthesis of muscarinic antagonist, PF-3635659 (I), is described, illustrating redesign of an analog-targeted synthesis which contained a scale-limiting rhodium-activated C-H amination step. The final route includes a reproducible modified Bouveault reaction which has not previously been reported on a substrate of this complexity, or on such a scale with over 5 kg of the requisite gem-dimethylamine prepared via this methodol. In the experiment, the researchers used many compounds, for example, Azetidin-3-ol hydrochloride(cas: 18621-18-6Related Products of 18621-18-6)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Related Products of 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson’s Disease Models》 was written by Kamakolanu, Uma Gayathri; Meyer, Michael E.; Yasuda, Dennis; Polgar, Willma E.; Marti, Matteo; Mercatelli, Daniela; Pisano, Clarissa Anna; Brugnoli, Alberto; Morari, Michele; Zaveri, Nurulain T.. Electric Literature of C3H8ClNO And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:

A novel series of C(3)-substituted piperdinylindoles were developed as nociceptin opioid receptor (NOP) partial agonists to explore a pharmacol. hypothesis that NOP partial agonists would afford a dual pharmacol. action of attenuating Parkinson’s disease (PD) motor symptoms and development of levodopa-induced dyskinesias. SAR around the C-3 substituents investigated effects on NOP binding, intrinsic activity, and selectivity and showed that while the C(3)-substituted indoles are selective, high affinity NOP ligands, the steric, polar, and cationic nature of the C-3 substituents affected intrinsic activity to afford partial agonists with a range of efficacies. Compounds 4, 5, and 9 with agonist efficacies between 25% and 35% significantly attenuated motor deficits in the 6-OHDA-hemilesioned rat model of PD. Further, unlike NOP antagonists, which appear to worsen dyskinesia expression, these NOP partial agonists did not attenuate or worsen dyskinesia expression. The NOP partial agonists and their SAR reported here may be useful to develop nondopaminergic treatments for PD. In addition to this study using Azetidin-3-ol hydrochloride, there are many other studies that have used Azetidin-3-ol hydrochloride(cas: 18621-18-6Electric Literature of C3H8ClNO) was used in this study.

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Electric Literature of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Synthetic Route of C3H8ClNOIn 2011 ,《Design of small molecule inhibitors of acetyl-CoA carboxylase 1 and 2 showing reduction of hepatic malonyl-CoA levels in vivo in obese Zucker rats》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Bengtsson, Christoffer; Blaho, Stefan; Saitton, David Blomberg; Brickmann, Kay; Broddefalk, Johan; Davidsson, Oejvind; Drmota, Tomas; Folmer, Rutger; Hallberg, Kenth; Hallen, Stefan; Hovland, Ragnar; Isin, Emre; Johannesson, Petra; Kull, Bengt; Larsson, Lars-Olof; Loefgren, Lars; Nilsson, Kristina E.; Noeske, Tobias; Oakes, Nick; Plowright, Alleyn T.; Schnecke, Volker; Stahlberg, Pernilla; Soerme, Pernilla; Wan, Hong; Wellner, Eric; Oester, Linda. The article conveys some information:

Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation Hybridization of weak inhibitors of ACC2 provided a novel, moderately potent but lipophilic series. Optimization led to two compounds, which exhibit potent inhibition of human ACC2, 10-fold selectivity over inhibition of human ACC1, good phys. and in vitro ADME properties and good bioavailability. X-ray crystallog. has shown this series binding in the CT-domain of ACC2 and revealed two key hydrogen bonding interactions. Both most potent compounds lower levels of hepatic malonyl-CoA in vivo in obese Zucker rats. The results came from multiple reactions, including the reaction of Azetidin-3-ol hydrochloride(cas: 18621-18-6Synthetic Route of C3H8ClNO)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Synthetic Route of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Product Details of 18621-18-6In 2020 ,《Discovery of a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins through the modulation of atropisomer interconversion properties》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Yamaguchi-Sasaki, Toru; Kawaguchi, Takanori; Okada, Atsushi; Tokura, Seiken; Tanaka-Yamamoto, Nozomi; Takeuchi, Tomoki; Ogata, Yuya; Takahashi, Ryo; Kurimoto-Tsuruta, Risa; Tamaoki, Tomokazu; Sugaya, Yutaka; Abe-Kumasaka, Tomoko; Arikawa, Kaho; Yoshida, Ippei; Sugiyama, Hiroyuki; Kanuma, Kosuke; Yoshinaga, Mitsukane. The article conveys some information:

The development of effective respiratory syncytial virus (RSV) fusion glycoprotein (F protein) inhibitors against both wild-type and the D486N-mutant F protein is urgently required. We recently reported a 15-membered macrocyclic pyrazolo[1,5-a]pyrimidine derivative 4 that exhibited potent anti-RSV activities against not only wild-type, but also D486N-mutant F protein. However, NMR studies revealed that the 15-membered derivative 4 existed as a mixture of atropisomers. An optimization study of the linker moiety between the 2-position of the benzoyl moiety and the 7-position of the pyrazolo[1,5-a]pyrimidine scaffold identified a 16-membered derivative 42c with an amide linker that showed a rapid interconversion of atropisomers. Subsequent optimization of the 5-position of the pyrazolo[1,5-a]pyrimidine scaffold and the 5-position of the benzoyl moiety resulted in the discovery of a potent clin. candidate 60b for the treatment of RSV infections. In addition to this study using Azetidin-3-ol hydrochloride, there are many other studies that have used Azetidin-3-ol hydrochloride(cas: 18621-18-6Product Details of 18621-18-6) was used in this study.

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Product Details of 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2015,Karlsson, Staffan; Bergman, Rolf; Loefberg, Christian; Moore, Peter R.; Ponten, Fritiof; Tholander, Joakim; Soerensen, Henrik published 《Development of a Large-Scale Route to an MCH1 Receptor Antagonist: Investigation of a Staudinger Ketene-Imine Cycloaddition in Batch and Flow Mode》.Organic Process Research & Development published the findings.SDS of cas: 18621-18-6 The information in the text is summarized as follows:

A practical large-scale route to an MCH1 receptor antagonist, azetidinyl oxadiazole I, is described. A Staudinger β-lactam synthesis of an imine and an in situ generated ketene was utilized as a key step for the preparation of a spiro-azetidine building block. The reaction was demonstrated in both batch and flow mode and a comparison of these techniques is described. In the experimental materials used by the author, we found Azetidin-3-ol hydrochloride(cas: 18621-18-6SDS of cas: 18621-18-6)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.SDS of cas: 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Application In Synthesis of Azetidin-3-ol hydrochlorideIn 2009 ,《Identification and Suppression of a Dimer Impurity in the Development of Delafloxacin》 appeared in Organic Process Research & Development. The author of the article were Hanselmann, Roger; Johnson, Graham; Reeve, Maxwell M.; Huang, Shu-Ting. The article conveys some information:

Delafloxacin is a 6-fluoroquinolone antibiotic which is under development at Rib-X Pharmaceuticals. During initial scale-up runs to prepare delafloxacin, up to 0.43% of a new impurity arose in the penultimate chlorination step. This was identified as a dimeric adduct I of delafloxacin. Subsequent application of design of experiments (DoE) led to the identification of the factors responsible for this impurity. Implementation of the knowledge gained from the DoE reproducibly enabled the suppression of this impurity to acceptable levels. In addition to this study using Azetidin-3-ol hydrochloride, there are many other studies that have used Azetidin-3-ol hydrochloride(cas: 18621-18-6Application In Synthesis of Azetidin-3-ol hydrochloride) was used in this study.

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Application In Synthesis of Azetidin-3-ol hydrochloride Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2018,Engelsma, Sander B.; van den Ende, Thomas C.; Overkleeft, Hermen S.; van der Marel, Gijsbert A.; Filippov, Dmitri V. published 《Reaction Rates of Various N-Acylenamines in the Inverse-Electron-Demand Diels-Alder Reaction》.European Journal of Organic Chemistry published the findings.Related Products of 18621-18-6 The information in the text is summarized as follows:

In light of the bioorthogonal inverse-electron-demand Diels-Alder strategy, an extended investigation into the effects of ring strain and electron inductive effects on the reactivity of the N-acylenamine core towards tetrazine has been carried out. Through a comparative study between N-acylazetines, N-vinylcarbamates and an N-vinylamide it was shown that ring strain has a more significant effect on reaction rate than electron donation. A significantly improved synthetic route is reported for the preparation of an N-acylazetine biorthogonal tag reported previously. The results came from multiple reactions, including the reaction of Azetidin-3-ol hydrochloride(cas: 18621-18-6Related Products of 18621-18-6)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Related Products of 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2007,Provins, Laurent; Christophe, Bernard; Danhaive, Pierre; Dulieu, Jacques; Gillard, Michel; Quere, Luc; Stebbins, Karin published 《Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives》.Bioorganic & Medicinal Chemistry Letters published the findings.SDS of cas: 18621-18-6 The information in the text is summarized as follows:

Introduction of 3-substituted azetidinyl substituents onto the 4,6-diaminopyrimidine scaffold allowed the improvement of PDE4 inhibiting activities. Preliminary in vivo activity in pulmonary inflammation models is reported.Azetidin-3-ol hydrochloride(cas: 18621-18-6SDS of cas: 18621-18-6) was used in this study.

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.SDS of cas: 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2018,El Awamy, Moustafa; Mohammad, Haroon; Hussien, Abdelrahman; Abutaleb, Nader S.; Hagras, Mohamed; Serya, Rabah A. T.; Taher, Azza T.; Abouzid, Khaled A. M.; Seleem, Mohamed N.; Mayhoub, Abdelrahman S. published 《Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens》.European Journal of Medicinal Chemistry published the findings.Product Details of 18621-18-6 The information in the text is summarized as follows:

With the continued rise of antibiotic resistance and reduced susceptibility to almost all front-line antibiotics, multidrug-resistant Gram-pos. bacterial infections represent an incessant threat to healthcare providers. This study presents a new series of phenylthiazole compounds where two active moieties were combined into one scaffold. The antibacterial activity of the hybrid structures extended to include several clin.-relevant multi-drug resistant pathogens including methicillin-resistant and vancomycin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, vancomycin-resistant enterococci, cephalosporin-resistant and methicillin-resistant Streptococcus pneumoniae, and Listeria monocytogenes. In addition, the most potent compounds, 16a and 17a, exhibited a fast bactericidal mode of action in vitro with low susceptibility to induce bacterial resistance. In addition to its potent spectrum of activity against Gram-pos. bacterial pathogens, compound 17a was found to be metabolically stable in rats, with a half-life of 4h. In the experimental materials used by the author, we found Azetidin-3-ol hydrochloride(cas: 18621-18-6Product Details of 18621-18-6)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Product Details of 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2018,Journal of the American Chemical Society included an article by Smith, Russell T.; Zhang, Xiaheng; Rincon, Juan A.; Agejas, Javier; Mateos, Carlos; Barberis, Mario; Garcia-Cerrada, Susana; de Frutos, Oscar; MacMillan, David W. C.. Computed Properties of C3H8ClNO. The article was titled 《Metallaphotoredox-Catalyzed Cross-Electrophile Csp3-Csp3 Coupling of Aliphatic Bromides》. The information in the text is summarized as follows:

A strategy for the installation of small alkyl fragments onto pharmaceutically relevant aliphatic structures has been established via metallaphotoredox catalysis. Herein, we report that tris(trimethylsilyl)silanol can be employed as an effective halogen abstraction reagent that, in combination with photoredox and nickel catalysis, allows a generic approach to Csp3-Csp3 cross-electrophile coupling. In this study, we demonstrate that a variety of aliphatic drug-like groups can be successfully coupled with a number of com. available small alkyl electrophiles, including Me tosylate and strained cyclic alkyl bromides. Moreover, the union of two secondary aliphatic carbon centers, a long-standing challenge for organic mol. construction, has been accomplished with a wide array of structural formats. Last, this technol. can be selectively merged with Csp2-Csp3 aryl-alkyl couplings to build drug-like systems in a highly modular fashion. The experimental part of the paper was very detailed, including the reaction process of Azetidin-3-ol hydrochloride(cas: 18621-18-6Computed Properties of C3H8ClNO)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Computed Properties of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts