【药物名称】CHAP-31
化学结构式(Chemical Structure):
参考文献No.45637
标题:Novel cyclic tetrapeptide derivs. and medicinal use thereof
作者:Mimoto, T.; Komatsu, Y.; Horinouchi, S.; Nishino, N.; Yoshida, M. (Japan Energy Corp.)
来源:EP 1010705; WO 9911659
合成路线图解说明:

The linear peptide-bound resin (VIII) was prepared by solid-phase synthesis on a Kaiser抯 oxime resin by sequential coupling-deprotection cycles with N-Boc-L-aminosuberic acid omega-benzyl ester (I), N-Boc-D-proline (III), N-Boc-L-isoleucine (V) and N-Boc-4-O-methyl-D-tyrosine (VII) to afford the peptide resins (II), (III), (IV) and (V), respectively. Cleavage of resin (VIII) with concomitant cyclization provided the cyclic tetrapeptide (IX). After hydrogenolysis of the side-chain benzyl ester, the resulting carboxylic acid was coupled to hydroxylamine in the presence of BOP and HOBt to obtain the title hydroxamic acid.

参考文献No.610393
标题:Synthesis and activity of Cyl-1 analogs having hydroxamic acid at side chain
作者:Tsukamoto, M.; et al.
来源:Pept Sci 1998,185
合成路线图解说明:

The linear peptide-bound resin (VIII) was prepared by solid-phase synthesis on a Kaiser抯 oxime resin by sequential coupling-deprotection cycles with N-Boc-L-aminosuberic acid omega-benzyl ester (I), N-Boc-D-proline (III), N-Boc-L-isoleucine (V) and N-Boc-4-O-methyl-D-tyrosine (VII) to afford the peptide resins (II), (III), (IV) and (V), respectively. Cleavage of resin (VIII) with concomitant cyclization provided the cyclic tetrapeptide (IX). After hydrogenolysis of the side-chain benzyl ester, the resulting carboxylic acid was coupled to hydroxylamine in the presence of BOP and HOBt to obtain the title hydroxamic acid.

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