反应详情

Analogously to Example 95) 4-[2-2(R)-amino-3-phenyl-propionylamino)-ethyl]-piperazine-1-carboxylic acid tert-butyl ester (obtained starting from Z-D-phenylalanine and N-Boc-4-hydroxyethylpiperazine by reactions and couplings widely described in literature and in part already reported in previous examples) (100 mg, 0.26 mmol) and 2-benzo[b]thiophen-2-yl-3-oxa-1-azaspiro[4.4]-non-1-en-4-one (72 mg, 0.26 mmol) are caused to react in DMF to yield a product which is deprotected and subsequently acylated with thiophen-2-yl-acethyl chloride in CH2Cl2 (as described in Example 94 and purified by flash chromatography using AcOEt as the eluent. 69 mg (0.10 mmol) of benzo[b]thiophene-2-carboxylic acid [1-(2-phenyl-1(R)-{2-[4-(thiophen-2-yl-acetyl)-piperazin-1-yl]-ethylcarbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide are so obtained.

1. customto yield a product which
2. custompurified by flash chromatography