L-164710

Chemical Name: 1-[5-(2,2-Diphenylacetyl)-1-(3,5-diphenylbenzyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-6(S)-ylcarbonyl]pyrrolidine-2(S)-carboxylic acid tert-butyl ester
项目整合开发状态: Biological Testing
项目研究机构: Merck & Co. (Originator)
合成路线:The reaction of 3-phenacyl-4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridine-6(S)-carboxylic acid methyl ester (I) with 2,2-diphenylacetic acid (II) gives 5-(2,2-diphenylacetyl)-3-phenacyl-4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridine-6(S)-carboxylic acid methyl ester (III),which is condensed with 3,5-dibromobenzyl bromide (IV) in acetic acid yielding the corresponding 1-(3,5-dibromobenzyl) derivative (V).The hydrolysis of the ester group of (V) with NaOH affords the expected free acid (VI),which is condensed with L-proline tert-butyl ester (VII) giving the corresponding N-substituted L-proline ester (VIII).Finall this compound is coupled with phenylboronic acid (IX),catalized with palladium tetrakis(triphenylphosphine) complex.