Anderson, Niall A. published the artcileSynthesis and determination of absolute configuration of a non-peptidic αvβ6 integrin antagonist for the treatment of idiopathic pulmonary fibrosis, Safety of 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid, the publication is Organic & Biomolecular Chemistry (2016), 14(25), 5992-6009, database is CAplus and MEDLINE.
A diastereoselective synthesis of I, a potential therapeutic agent for the treatment of idiopathic pulmonary fibrosis, which is currently undergoing Phase I trials is reported. The key steps in the synthesis involved alkylation of 2-methylnaphthyridine with (R)-N-Boc-3-(iodomethyl)-pyrrolidine, and an asym. Rh-catalyzed addition of an arylboronic acid to a 4-(N-pyrrolidinyl)crotonate ester. The overall yield of the seven linear step synthesis is 8% and the product is obtained in <99.5% ee proceeding with 80% de. The absolute configuration of I is established by an alternative asym. synthesis involving alkylation of an arylacetic acid using Evans oxazolidinone chem., acylation using the resulting 2-arylsuccinic acid, and reduction The absolute configuration of the benzylic asym. center is established as (S).
Organic & Biomolecular Chemistry published new progress about 1025735-46-9. 1025735-46-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Benzene,Boronic Acids, name is 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid, and the molecular formula is C11H13BN2O2, Safety of 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid.
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