557101-39-0

Upstream product

• 50-00-0 formaldehyd 
• 5526-36-3 3-oxo-glutaric acid monoethyl ester 
• 52244-03-8 ethyl 3-(1-(2-ethoxy-2-oxoethyl)-6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)propanoate 
• 5911-33-1 ethyl 9,10-dimethoxy-2-oxo-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinoline-3-carboxylate 

Downstream Products

• 1012065-72-3 (S)-2-amino-9,10-dimethoxy-1,6,7,11b-tetrahydro-4H-pyrido[2,1-a]isoquinoline-3-carboxylic acid ethyl ester, (S,S)-2,3-bisbenzoyloxysuccinic acid salt 
• 1012065-68-7 (S)-2-amino-9,10-dimethoxy-1,6,7,11b-tetrahydro-4H-pyrido[2,1-a]isoquinoline-3-carboxylic acid ethyl ester (2S,3S)-bis-benzyloxy-N,N-dimethyl-succinamic acid salt 

Relevant academic research and scientific papers

An efficient process for the manufacture of carmegliptin

A short and high-yielding synthesis of carmegliptin (1) suitable for large-scale production is reported. The tricyclic core was assembled efficiently by a decarboxylative Mannich addition-Mannich cyclization sequence. Subsequent crystallization-induced dynamic resolution of enamine 7 using (S,S)-dibenzoyltartaric acid was followed by diastereoselective enamine reduction to give the fully functionalized tricyclic core with its three stereogenic centers. The C-3 nitrogen was introduced by Hofmann rearrangement of amide 28, and the resulting amine 10 was coupled with (S)-fluoromethyl lactone 31. Following cyclization to lactam 13 and amine deprotection, 1 was obtained in 27-31% overall yield with six isolated intermediates.

PROCESS FOR THE PREPARATION OF PYRIDO [2,1-a] ISOQUINOLINE DERIVATIVES COMPRISING OPTICAL RESOLUTION OF AN ENAMINE

This invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an

PROCESS FOR THE PREPARATION OF PYRIDO [ 2-1-A] ISOQUINOLINE DERIVATIVES BY CATALYTIC ASYMMETRIC HYDROGENATION OF AN ENAMINE

The invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula wherein R2, R3and R4 are as defined in the specification, comprising the steps of a) catalytic asymmetric hydr

Pyrido [2,1-a] isoquinoline derivatives

The present invention relates to compounds of formula (I) wherein R1 is as defined in the description, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated

Pyrido [2,1-a] isoquinoline derivatives

The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as indicated in the description, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of

Pyrido [2,1-a] isoquinoline derivatives

The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds a