882435-40-7

Upstream product

• 162537-11-3 (S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoic acid 
• 872703-72-5 (2S)-2-benzyl-oxirane-N-[(1S,2R)-2-hydroxy-indan-1-yl]-2-carboxylic acid amide 
• 882435-39-4 {(1S)-1-[N'-(3-bromo-benzyl)hydrazinocarbonyl]-2,2-dimethyl-propyl}carbamic acid methyl ester 
• 51859-95-1 3-bromobenzylhydrazine 

Relevant academic research and scientific papers

Microwave-accelerated synthesis of P1′-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold

Two series of P1′-extended HIV-1 protease inhibitors comprising a tertiary alcohol in the transition-state mimic exhibiting Ki values ranging from 2.1 to 93 nM have been synthesized. Microwave-accelerated palladium-catalyzed cross-couplings were utilized to rapidly optimize the P1′ side chain. High cellular antiviral potencies were encountered when the P1′ benzyl group was elongated with a 3- or 4-pyridyl substituent (EC50 = 0.18-0.22 μM). X-ray crystallographic data were obtained for three inhibitors cocrystallized with the enzyme.

HIV protease inhibitors

Compounds of the formula (I): Wherein R1, R2, X and N are as defined in the specification; E is N, CH; A1 and A" are terminal groups as defined in the specification. The compounds have utility as HIV-I protease inhibitors.