Category: 18621-18-6

Synthetic Route of C3H8ClNOIn 2020 ,《Design, optimization, and study of small molecules that target tau pre-mRNA and affect splicing》 was published in Journal of the American Chemical Society. The article was written by Chen, Jonathan L.; Zhang, Peiyuan; Abe, Masahito; Aikawa, Haruo; Zhang, Liying; Frank, Alexander J.; Zembryski, Timothy; Hubbs, Christopher; Park, Ha Jeung; Withka, Jane; Steppan, Claire; Rogers, Lucy; Cabral, Shawn; Pettersson, Martin; Wager, Travis T.; Fountain, Matthew A.; Rumbaugh, Gavin; Childs-Disney, Jessica L.; Disney, Matthew D.. The article contains the following contents:

Approx. 95% of human genes are alternatively spliced, and aberrant splicing events can cause disease. One pre-mRNA that is alternatively spliced and linked to neurodegenerative diseases is tau (microtubule-associated protein tau), which can cause frontotemporal dementia and parkinsonism linked to chromosome 17 (FTDP-17) and can contribute to Alzheimer′s disease. Here, we describe the design of structure-specific lead small mols. that directly target tau pre-mRNA from sequence. This was followed by hit expansion and analog synthesis to further improve upon these initial lead mols. The emergent compounds were assessed for functional activity in a battery of assays, including binding assays and an assay that mimics mol. recognition of tau pre-mRNA by a U1 small nuclear ribonucleoprotein (snRNP) splicing factor. Compounds that emerged from these studies had enhanced potency and selectivity for the target RNA relative to the initial hits, while also having significantly improved drug-like properties. The compounds are shown to directly target tau pre-mRNA in cells, via chem. crosslinking and isolation by pull-down target profiling, and to rescue disease-relevant splicing of tau pre-mRNA in a variety of cellular systems, including primary neurons. More broadly, this study shows that lead, structure-specific compounds can be designed from sequence and then further optimized for their physicochem. properties while at the same time enhancing their activity. 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

In 2012,Roughley, Stephen D.; Browne, Helen; Macias, Alba T.; Benwell, Karen; Brooks, Teresa; D’Alessandro, Jalanie; Daniels, Zoe; Dugdale, Sarah; Francis, Geraint; Gibbons, Ben; Hart, Terance; Haymes, Timothy; Kennett, Guy; Lightowler, Sean; Matassova, Natalia; Mansell, Howard; Merrett, Angela; Misra, Anil; Padfield, Anthony; Parsons, Rachel; Pratt, Robert; Robertson, Alan; Simmonite, Heather; Tan, Kiri; Walls, Steven B.; Wong, Melanie published 《Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity》.Bioorganic & Medicinal Chemistry Letters published the findings.HPLC of Formula: 18621-18-6 The information in the text is summarized as follows:

Attempts to optimize the human fatty acid amide hydrolase (FAAH) inhibition and physicochem. properties of previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084, are reported. The SAR of a series of analogs and in vivo dose-dependent FAAH inhibition in an anandamide-loading study in rats were determined The experimental part of the paper was very detailed, including the reaction process of Azetidin-3-ol hydrochloride(cas: 18621-18-6HPLC of Formula: 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.HPLC of Formula: 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,Firth, Nicholas C.; Atrash, Butrus; Brown, Nathan; Blagg, Julian published 《MOARF, an Integrated Workflow for Multiobjective Optimization: Implementation, Synthesis, and Biological Evaluation》.Journal of Chemical Information and Modeling published the findings.Computed Properties of C3H8ClNO The information in the text is summarized as follows:

We describe the development and application of an integrated, multiobjective optimization workflow (MOARF) for directed medicinal chem. design. This workflow couples a rule-based mol. fragmentation scheme (SynDiR) with a pharmacophore fingerprint-based fragment replacement algorithm (RATS) to broaden the scope of reconnection options considered in the generation of potential solution structures. Solutions are ranked by a multiobjective scoring algorithm comprising ligand-based (shape similarity) biochem. activity predictions as well as physicochem. property calculations Application of this iterative workflow to optimization of the CDK2 inhibitor Seliciclib (CYC202, R-roscovitine) generated solution mols. in desired physicochem. property space. Synthesis and exptl. evaluation of optimal solution mols. demonstrates CDK2 biochem. activity and improved human metabolic stability. 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

Recommanded Product: Azetidin-3-ol hydrochlorideIn 2021 ,《Asymmetric copper-catalyzed propargylic amination with amine hydrochloride salts》 appeared in Chemical Communications (Cambridge, United Kingdom). The author of the article were Huang, Jian; Kong, Han-Han; Li, Si-Jia; Zhang, Rui-Jin; Qian, Hao-Dong; Li, Dan-Ran; He, Jin-Yu; Zheng, Yi-Nuo; Xu, Hao. The article conveys some information:

The highly enantioselective copper-catalyzed propargylic amination of propargylic esters with amine hydrochloride salts has been realized for the first time using copper salts with chiral N,N,P-ligands. This method features a broad substrate scope and wide functional group tolerance, generating propargylic amines in good to excellent yields with high enantioselectivities (up to 99% ee). The utility of the approach was demonstrated by late-stage functionalization of marketed pharmaceuticals. In the experimental materials used by the author, we found Azetidin-3-ol hydrochloride(cas: 18621-18-6Recommanded Product: Azetidin-3-ol hydrochloride)

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.Recommanded Product: 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 2010,Krishna Reddy, V. V. R. M.; Kishore Babu, K.; Ganesh, A.; Srinivasulu, P.; Madhusudhan, G.; Mukkanti, K. published 《Improved Process for the Preparation of 1-Benzhydrylazetidin-3-ol: Development of an Efficient Synthesis and Identification of Process-related Impurities and/or Intermediates》.Organic Process Research & Development published the findings.Application In Synthesis of Azetidin-3-ol hydrochloride The information in the text is summarized as follows:

An improved, one-pot, and multikilogram-scale synthesis of 1-benzhydrylazetidin-3-ol, the pharmaceutically important moiety, has been developed. The improved process for the preparation of 1-benzhydrylazetidin-3-ol was able to minimize a content of impurities and allows the effective production of 1-benzhydrylazetidin-3-ol and its scale-up. The process was high yielding (80%) and chromatog.-free with purity 99.3 area %.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 2011,Krishna Reddy, V. V. R. M.; Udaykiran, D.; Chintamani, U. S.; Mahesh Reddy, E.; Kameswararao, Ch.; Madhusudhan, G. published 《Development of an optimized process for the preparation of 1-Benzylazetidin-3-ol: an industrially important intermediate for substituted azetidine》.Organic Process Research & Development published the findings.Name: Azetidin-3-ol hydrochloride The information in the text is summarized as follows:

A thoroughly optimized and robust process for the synthesis of 1-benzylazetidin-3-ol has been emphasized. 1-Benzylazetidin-3-ol I, has been utilized as a starting material in the com. synthesis of azetidin-3-ol hydrochloride. Synthesis of azetidin-3-ol hydrochloride involves the usage of very low cost and com. available starting material (benzylamine) and with reduced formation of di(3-chloro-2-hydroxypropyl) benzylamine significantly resulting in an economical process that allows the effective production of 1-benzyl azetidin-3-ol as well as azetidin-3-ol hydrochloride. In the experiment, the researchers used Azetidin-3-ol hydrochloride(cas: 18621-18-6Name: Azetidin-3-ol hydrochloride)

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.Name: 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 2012,Davis, Tyler A.; Danneman, Michael W.; Johnston, Jeffrey N. published 《Chiral proton catalysis of secondary nitroalkane additions to azomethine: synthesis of a potent GlyT1 inhibitor》.Chemical Communications (Cambridge, United Kingdom) published the findings.Application In Synthesis of Azetidin-3-ol hydrochloride The information in the text is summarized as follows:

The first enantioselective synthesis of a potent GlyT1 inhibitor is described. A 3-nitroazetidine donor is used in an enantioselective aza-Henry reaction catalyzed by a bis(amidine)-triflic acid salt organocatalyst, delivering the key intermediate with 92% ee. This adduct is reductively denitrated and converted to the target through a short sequence, thereby allowing assignment of the absolute configuration of the more potent enantiomer. In the experiment, the researchers used Azetidin-3-ol hydrochloride(cas: 18621-18-6Application In Synthesis of Azetidin-3-ol hydrochloride)

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 2017,Maxwell, Brad D. published 《The syntheses of [13C6] and [phenyl-14C(U)]BMS-816336, an inhibitor of 11β-hydroxysteroid dehydrogenase type 1, for type 2 diabetes》.Journal of Labelled Compounds and Radiopharmaceuticals published the findings.HPLC of Formula: 18621-18-6 The information in the text is summarized as follows:

Type 2 diabetes is a significant worldwide health problem. To support the development of BMS-816336 as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 for type 2 diabetes, the synthesis of carbon-14 labeled material was required for use in metabolic profiling. [Phenyl-14C(U)]BMS-816336 (A) was synthesized in 8 steps and 22% radiochem. yield from com. available [14C(U)]bromobenzene. The radiochem. purity of A was 100% having a specific activity of 84.4 μCi/mg or 28.8 mCi/mmol for a total of 8.9 mCi. It was also necessary to synthesize [13C6]BMS-816336 (B) for use as a liquid chromatog./mass spectrometry standard B was also prepared in 8 labeled steps in 26% yield from [13C6]bromobenzene. In the experiment, the researchers used many compounds, for example, Azetidin-3-ol hydrochloride(cas: 18621-18-6HPLC of Formula: 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.HPLC of Formula: 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 2022,Koike, Tatsuki; Constantinescu, Cristian C.; Ikeda, Shuhei; Nishi, Toshiya; Sunahara, Eiji; Miyamoto, Maki; Cole, Patricia; Barret, Olivier; Alagille, David; Papin, Caroline; Morley, Thomas; Fowles, Krista; Seibyl, John; Tamagnan, Gilles; Kuroita, Takanobu published an article in European Journal of Nuclear Medicine and Molecular Imaging. The title of the article was 《Preclinical characterization of [18F]T-008, a novel PET imaging radioligand for cholesterol 24-hydroxylase》.Recommanded Product: 18621-18-6 The author mentioned the following in the article:

Cholesterol 24-hydroxylase (CH24H) is a brain-specific enzyme that plays a major role in brain cholesterol homeostasis by converting cholesterol into 24S-hydroxycholesterol. The selective CH24H inhibitor soticlestat (TAK-935) is being pursued as a drug for treatment of seizures in developmental and epileptic encephalopathies. Herein, we describe the successful discovery and the preclin. validation of the novel radiolabeled CH24H ligand (3-[18F]fluoroazetidin-1-yl){1-[4-(4-fluorophenyl)pyrimidin-5-yl]piperidin-4-yl}methanone ([18F]T-008) and its tritiated analog, [3H]T-008. In vitro autoradiog. (ARG) studies in the CH24H wild-type (WT) and knockout (KO) mouse brain sections were conducted using [3H]T-008. PET imaging was conducted in two adult rhesus macaques using [18F]T-008. Each macaque received two test-retest baseline scans and a series of two blocking doses of soticlestat administered prior to [18F]T-008 to determine the CH24H enzyme occupancy. PET data were analyzed with Logan graphical anal. using plasma input. A Lassen plot was applied to estimate CH24H enzyme occupancy by soticlestat. In ARG studies, binding of [3H]T-008 was specific to CH24H in the mouse brain sections, which was not observed in CH24H KO or in wild-type mice after pretreatment with soticlestat. In rhesus PET studies, the rank order of [18F]T-008 uptake was striatum > cortical regions > cerebellum, which was consistent with CH24H distribution in the brain. Pre-blocking with soticlestat reduced the maximum uptake and increased the washout in all brain regions in a dose-dependent manner. Calculated global occupancy values for soticlestat at a dose of 0.89 mg/kg were 97-98%, indicating maximum occupancy. The preclin. in vitro and in vivo evaluation of labeled T-008 demonstrates that [18F]T-008 is suitable for imaging CH24H in the brain and warrants further studies in humans. In the experimental materials used by the author, we found Azetidin-3-ol hydrochloride(cas: 18621-18-6Recommanded Product: 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.Recommanded Product: 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