125075-98-1

Upstream product

• 125016-02-6 Benzyl 2(R)-(4-methoxybenzyl)-3-(morpholinocarbonyl)-propionate 
• 125016-01-5 3-<1,4-dioxo-2-(R)-(4-methoxybenzyl)-4-morpholinobutyl>-4-(S)-isopropyl-2-oxazolidinone 

Downstream Products

• 132094-08-7 (2R,4S,5S)-N-butyl-6-cyclohexyl-4-hydroxy-5-{N-[2(R)-(4-methoxybenzyl)-3-(morpholinocarbonyl)propionyl]-3-(4-thiazolyl)-L-alanyl}amino-2-methylhexanamide 
• 132094-04-3 (2S,4S,5S)-5-{N-[2(R)-(4-methoxybenzyl)-3-(morpholinocarbonyl)propionyl]-3-(4-thiazolyl)-L-alanyl}amino-6-cyclohexyl-4-hydroxy-2-isopropyl-N-methylhexanamide 

Relevant academic research and scientific papers

RENIN-INHIBITORY OLIGOPEPTIDES, THEIR PREPARATION AND USE

Compounds of formula (I): STR1 A is a carbon-carbon bond or C 1-C 3 alkylene; B is imino group or C 1-C 2 alkylene; R 1 is C 1-C 4 alkyl, C 1-C 4 alkoxy, heterocyclic or optionally substituted amino; R 2 is optionally substituted phenyl or optionally substituted naphthyl; R 3 is thiazolyl, isoxazolyl or imidazolyl; R 4 is isopropyl or cyclohexyl; R 5 and R 6 are C. sub.1-C 4 alkyl, or, together with the carbon atom to which they are attached, C 3-C 7 cycloalkyl; R. sup.7 is hydrogen, optionally substituted C 1-C 6 alkyl group; and R 8 is hydrogen or C. sub.1-C 4 alkyl. These compounds have renin-inhibitory and, hence, hypotensive activities. The invention also provides a method for the treatment or prophylaxis of hypertension induced by failures in the renin-angiotensin system.

Asymmetric synthesis of 2-substituted-3-aminocarbonyl propionic acid.

An asymmetric synthetic route to 2-substituted-3-aminocarbonyl propionic acid, which is the significant component of low-molecular-weight renin inhibitors, is described. The key step of this synthesis is diastereoselective alkylation by using chiral oxazo