122535-03-9Relevant articles and documents
Synthesis method for 4-(tert-butoxycarbonyl) octahydrofuro[3,2-b] pyridine-6-carboxylic acid
-
Paragraph 0008; 0025; 0026, (2016/12/16)
The present incention relates to a synthesis method for 4-(tert-butoxycarbonyl) octahydrofuro[3,2-b] pyridine-6-carboxylic acid, and mainly solves the technical problem of no synthesis method suitable for industrialization at present. The synthesis method comprises six steps: first esterifying a compound 1 to obtain a compound 2; then performing iodination to produce a compound 3; acetylating the compound 3 to obtain a compound 4; then performing coupling to obtain a compound 5; performing cyclization to obtain a compound 6; performing hydrogenation to obtain a compound 7, then reacting with Boc anhydride to obtain a compound 8; and performing hydrogenation to obtain a final compound 9. The reaction formula is shown in the description.
Identification of MK-944a: A second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors
Dorsey,McDonough,McDaniel,Levin,Newton,Hoffman,Darke,Zugay-Murphy,Emini,Schleif,Olsen,Stahlhut,Rutkowski,Kuo,Lin,Chen,Michelson,Holloway,Huff,Vacca
, p. 3386 - 3399 (2007/10/03)
Recent results from human clinical trials have established the critical role of HIV protease inhibitors in the treatment of acquired immune-deficiency syndrome (AIDS). However, the emergence of viral resistance, demanding treatment protocols, and adverse side effects have exposed the urgent need for a second generation of HIV protease inhibitors. The continued exploration of our hydroxylaminepentanamide (HAPA) transition-state isostere series of HIV protease inhibitors, which initially resulted in the identification of Crixivan (indinavir sulfate, MK-639, L-735,524), has now yielded MK-944a (L-756,423). This compound is potent, is selective, and competitively inhibits HIV-1 PR with a K(i) value of 0.049 nM. It stops the spread of the HIV(IIIb)-infected MT4 lymphoid cells at 25.0-50.0 nM, even in the presence of α1 acid glycoprotein, human serum albumin, normal human serum, or fetal bovine serum. MK-944a has a longer half-life in several animal models (rats, dogs, and monkeys) than indinavir sulfate and is currently in advanced human clinical trials.
Furopyridine sulfonamides and their opthalmological compositions
-
, (2008/06/13)
Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.