تفاعل #78214

معادلة التفاعل

methyl 2-acetamido-3-[2-[(2R)-2-[[3-(4-aminophenyl)benzoyl]amino]-4-benzyloxycarbonylbutoxy]-4-cyanophenyl]acrylate trifluoroacetate

chloroformamidine hydrochloride

dimethyl sulfone

→

title compound

Methyl 2-acetamido-3-[2-[(2R)-2-[[3-(4-guanidinophenyl)benzoyl]amino]-4-benzyloxycarbonylbutoxy]-4-cyano-phenyl]acrylate trifluoroacetate

المذيبات

Water

ظروف التفاعل

المعالجة

1. 1
   غسيلAfter washing with ethyl acetate
2. 2
   أخرىthe aqueous layer was freeze-dried
3. 3
   أخرىpurified by the reversed phase HPLC in the same manner as that in step 5 in Example 1

الإجراء التجريبي

A mixture of 340 mg (0.52 mmol) of methyl 2-acetamido-3-[2-[(2R)-2-[[3-(4-aminophenyl)benzoyl]amino]-4-benzyloxycarbonylbutoxy]-4-cyanophenyl]acrylate trifluoroacetate, 430 mg (3.74 mmol) of chloroformamidine hydrochloride and 2.0 g of dimethyl sulfone was stirred at 120° C. for 2 hours. Water was added to the reaction mixture. After washing with ethyl acetate, the aqueous layer was freeze-dried and purified by the reversed phase HPLC in the same manner as that in step 5 in Example 1 to obtain the title compound.

المصدر