NCO-700

Chemical Name: Bis[ethyl(2R,3R)-trans-3-[(S)-3-methyl-1-[4-(2,3,4-trimethoxybenzyl)piperazin-1-ylcarbonyl]butylcarbamoyl]oxyran-2-carboxylate]sulfate; [2R-[2alpha,3beta(S*)]]-3-[[[3-Methyl-1-[[4-[(2,3,4-trimethoxyphenyl)methyl]-1-piperazinyl]carbonyl]butyl]amino]carbonyl]oxiranecarboxylic acid ethyl ester sulfate (2:1)
CAS No. 84579-82-8
项目整合开发状态: Phase II
项目研究机构: Nippon Chemiphar (Originator)
合成路线:The condensation of N-(tert-butoxycarbonyl)-L-leucine (I) with 1-2,3,4-trimethoxybenzyl)piperazine (II) by means of N-hydroxysuccinimide (HSI) and dicyclohexylcarbodiimide (DCC) in dichloromethane gives the corresponding acylated piperazine (III),which is deprotected with dry HCl in ethyl acetate yielding the leucine derivative (IV).Finally,this compound is condensed with trans-epoxysuccinic acid monoethyl ester (V) by means of DCC and HSI as before and treated with H2SO4.

合成路线:The reaction of 1-(1-propen-2-yl)-2 benzimidazolinone (I) in hexamethylphosphorus triamide with sodium hydride and 3-benzalamino-3,3-dimethylpropyl chloride (II) and treating the reaction product with hydrochloric acid gives 1-(3 amino-3,3-dimethylpropyl)-2 benzimidazolone (III).The amine (III) is refluxed with 1-(1-naphthyloxy)propylene-(2,3)-oxide (IV) yielding the title compound.