【药物名称】MRS-2286
化学结构式(Chemical Structure):
参考文献No.567501
标题:Acyclic analogues of deoxyadenosine 3',5'-bisphosphates as P2Y1 receptor antagonists
作者:Kim, Y.C.; Gallo-Rodriguez, C.; Jang, S.Y.; Nandanan, E.; Adams, M.; Harden, T.K.; Boyer, J.L.; Jacobson, K.A.
来源:J Med Chem 2000,43(4),746
合成路线图解说明:

The sodium salt of triethyl methanetricarboxylate (I) was alkylated with 1,2-dibromoethane (II) to afford bromide (III). Subsequent condensation of 6-(methylamino)-2-chloropurine (IV) with bromide (III) in the presence of K2CO3 gave adduct (V). Mono-decarbethoxylation of tricarboxylate (V) upon treatment with NaOMe produced malonate (VI), which was further reduced to diol (VII) by means of NaBH4 in CH2Cl2-MeOH. Treatment of (VII) with tetrabenzyl pyrophosphate in the presence of LDA gave rise to the bis-phosphate ester (VIII). The benzyl groups of (VIII) were then cleaved employing boron trichloride, and the resulting phosphoric acid was purified through an ion-exchange resin in the presence of ammonium bicarbonate to furnish the title tetraammonium salt.

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