On April 22, 2004, Lowe, John A.; Volkmann, Robert A. published a patent.Formula: C3H10ClNO The title of the patent was Preparation of 2-amino-6-(2,4,5-substituted-phenyl)pyridines as nitrous oxide synthase (NOS) inhibitors. And the patent contained the following:
Title compounds I [R1 = Me, Et, Pr, etc.; R2 = H, Me, Et, Pr, etc.; m = 1-3; R3-4 = Ph, 5-6-membered heteroaryl containing from 1 to 4 heteroatoms, etc.] are prepared For instance, 4-benzyloxy-5-ethyl-2-methoxyphenylboronic acid (preparation given) is reacted with 2-bromo-6-(2,5-dimethylpyrrol-1-yl)pyridine (EtOHaq, Na2CO3, (PPh3)4Pd, reflux, 64 h) and the resulting adduct debenzylated (MeOH, NH4O2CH, Pd(OH)2, reflux, 45 min), the amino residue unmasked (EtOHaq, NH2OH, reflux, 16 h), alkylated with 3-((methanesulfonyl)oxy)azetidine-1-carboxylic acid tert-Bu ester (DMSO, t-BuOK) and finally converted to II (THF, LAH). Example compounds exhibit IC50 < 1 μM for inhibition of NOS. I are useful for the treatment of treatment and prevention of central nervous system and other disorders. I are also used for inhibiting neurol. damage caused by impairment of glucose and/or oxygen to the brain; in one embodiment, the NOS inhibitor is administered to the mammal prior to surgery, e.g., prior to cardiac surgery, angioplasty, or angiog. The experimental process involved the reaction of 2-(Methylamino)ethan-1-ol hydrochloride(cas: 62640-03-3).Formula: C3H10ClNO
The Article related to amino phenyl pyridine nitric oxide synthase inhibitor preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Formula: C3H10ClNO
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