1007392-69-9

Upstream product

• 1206625-73-1 (3'R,4'S)-3'-{[2-chloro-5-(2-methoxy-ethyl)-benzyl]cyclopropylcarbamoyl}-6-[2-(2,6-dichloro-4-methyl-phenoxy)ethoxy]-3',4',5',6'-tetrahydro-2'H-[3,4']bipyridinyl-1'-carboxylic acid tert-butyl ester 
• 921630-23-1 N-[2-chloro-5-(2-methoxyethyl)benzyl]cyclopropanamine 
• 945999-98-4 5-bromo-2-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]pyridine 
• 1265907-54-7 6-[2-(2,6-dichloro-4-methyl-phenoxy)ethoxy]-5',6'-dihydro-2'H-[3,4']bipyridinyl-1',3'-dicarboxylic acid 1'-tert-butyl ester 3'-ethyl ester 
• 1206625-88-8 6-[2-(2,6-dichloro-4-methyl-phenoxy)ethoxy]-1'-(2,2,2-trifluoroacetyl)-1',2',5',6'-tetrahydro-[3,4']bipyridinyl-3'-carboxylic acid ethyl ester 
• 1265907-55-8 (3'S,4'S)-6-[2-(2,6-dichloro-4-methyl-phenoxy)ethoxy]-3',4',5',6'-tetrahydro-2'H-[3,4']bipyridinyl-1',3'-dicarboxylic acid 1'-tert-butyl ester 3'-ethyl ester 
• 1206625-70-8 C₂₄H₂₅Cl₂F₃N₂O₅ 
• 1206625-81-1 2-chloro-5-formylbenzoic acid 
• 1206625-83-3 2-chloro-5-(2-methoxyvinyl)benzoic acid 
• 1206625-85-5 2-chloro-5-(2-methoxyethyl)benzoic acid 
• 1206625-87-7 2-chloro-N-cyclopropyl-5-(2-methoxyethyl)benzamide 
• 1206625-60-6 2-[2-(2,6-dichloro-4-methyl-phenoxy)ethoxy]-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)pyridine 
• 1246643-49-1 C₁₀H₁₂F₃NO₄ 
• 1206625-66-2 1-(2,2,2-trifluoro-acetyl)-4-trifluoromethanesulfonyloxy-1,2,5,6-tetrahydro-pyridine-3-carboxylic acid ethyl ester 

Downstream Products

• 1206625-79-7 (3'R,4'S)-6-[2-(2,6-dichloro-4-methyl-phenoxy)ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)benzyl]cyclopropylamide acetate 

Relevant academic research and scientific papers

A practical synthesis of renin inhibitor MK-1597 (ACT-178882) via catalytic enantioselective hydrogenation and epimerization of piperidine intermediate

A practical enantioselective synthesis of renin inhibitor MK-1597 (ACT-178882), a potential new treatment for hypertension, is described. The synthetic route provided MK-1597 in nine steps and 29% overall yield from commercially available p-cresol (7). The key features of this sequence include a catalytic asymmetric hydrogenation of a tetrasubstituted ene-ester, a highly efficient epimerization/saponification sequence of 4 which sets both stereocenters of the molecule, and a short synthesis of amine fragment 2.

Piperidine-based renin inhibitors: Upper chain optimization

The optimization of the 4-position of recently described new 3,4-disubstituted piperidine-based renin inhibitors is reported herein. The synthesis and characterization of compounds leading to the discovery of 11 (ACT-178882, MK-1597), a renin inhibitor wi

PROCESS FOR MAKING A RENIN INHIBITOR

A salt of the compound (3'R,4'S)-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide selected from the group consisting of monoacetate salt and bis-D-tartrate salt. In one embodiment of the invention, the salt is (3',4'S)-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide monoacetate. In one embodiment of the invention, the salt is (3'R, 4'S)-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide bis-D-tartrate. The invention also describes a asymmetric synthesis of (3'R, 4'S)-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide as a monoacetate salt or as a bis-D-tartrate salt

Novel Piperidine Carboxylic Acid Amide Derivatives

The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these