Leupeptine und ihre Analoga

摘要

1292846 Leupeptins ZAIDAN HOJIN BISEIBUTSU KAGAKO KENKYU KAI 10 Nov 1969 [21 Nov 1968 30 Nov 1968 11 June 1969] 54834/69 Heading C2C Compounds (I) (wherein n is 1 or 0; R 3 is Me or Et and R 1 and R 2 are CHMe 2 , CH 2 CHMe 2 or CH(Me)(Et) are prepared by reducing a compound (II) with a metal hydride at room temperature to 150‹ C. to give a compound (III) and oxidizing this with sulphoxide-carbodiimide at room temperature, or by reacting (II) with thionyl chloride to give the acid chloride and reducing this with hydrogen in the presence of a hydrogenation catalyst at 120-30‹ C: The following starting materials were prepared: Z-Leu-Leu-OEt, and -OH, Z-Leu-Leu- Arg(NO 2 )OMe, H - Leu - Leu - Arg - OMediHOAc, Ac - Leu - Leu - ArgOMe and - OH; Pr - Leu - Leu - ArgOH; Ac - Leu - Leu - ArgCl, HCl; Z - Leu - Arg(NO 2 )OMe, HLeu - Arg- OMediHOAc, and Ac - Leu - Arg - OMe and -OH.