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【结 构 式】

【分子编号】34503

【品名】 

【CA登记号】

【 分 子 式 】C59H77N11O11S2

【 分 子 量 】1180.45992

【元素组成】C 60.03% H 6.57% N 13.05% O 14.91% S 5.43%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(XII)

The resin (X) was coupled with N-Boc-L-phenylalanine (XI) affording resin (XII). The acetylation of the free amino group, side-chain deprotection and cleavage from the resin (XII) employing liquid HF and p-cresol yielded the linear dipeptide (XIII). This was finally cyclized with benzotriazol-1-yloxytris (dimethylamino)phosphonium hexafluorophosphate (BOP) to produce the title cyclic peptide.

1 Wong, A.K.; Finch, A.M.; Pierens, G.K.; Craik, D.J.; Taylor, S.M.; Fairlie, D.P.; Small molecular probes for G-protein-coupled C5a receptors: Conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a. J Med Chem 1998, 41, 18, 3417.
2 Wong, A.K.; Fairlie, D.P.; Finch, A.M.; Wadi, S.K.; Craik, D.J.; Taylor, S.M.; Paczkowski, N.J.; Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem 1999, 42, 11, 1965.
3 Fairlie, D.; Wong, A.; Finch, A.M.; Taylor, S.M. (University of Queensland); Cyclic agonists and antagonists of C5a receptors and G protein-coupled receptors. EP 1017713; WO 9900406 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(X) 34502   C50H68N10O10S2 详情 详情
(XI) 12874 (2R)-2-[(tert-Butoxycarbonyl)amino]-3-phenylpropionic acid; N-alpha-t-BOC-L-Phenylalanine 13734-34-4 C14H19NO4 详情 详情
(XII) 34503   C59H77N11O11S2 详情 详情
(XIII) 34504   C47H67N11O8 详情 详情
Extended Information