| 主权项 |
1. A process for preparing the compound which comprises: (a) reacting the compound 1with the acid chloride compoundto form the compound 2and then
(b) contacting the compound 2 with a di-substituted amine (R2)2NH in base to produce the compound 3and thereafter
(c) reacting the compound 3 with the dihydroxy compoundin acid solution, wherein the linker between the hydroxyl groups is C1-C6 alkyl, to yield the compound 4and
(d) reacting the compound 4 with the compoundin acid to produce the compound 5 (e) contacting the compound 5 with Me-X4 in base or MeO—R3 in acid to produce the compound 6and
(f) then performing an oxidation reaction on compound 6 to yield compound 7and
(g) adding the triazolyl groupto compound 7, and then conducting a functional group interconversion reaction, to obtain the compound (I) above wherein:
R1═—H, -Boc, -Piv, —SO2Aryl, —CH2SAryl, —CH2OP(O)(OR)2, —CH2OR, —CH2Aryl;R2=each independently —H, —CO2R, —SO2Aryl, —CHO;R3 and R4=each independently —H, —CO2R, —CH2SR, —CH2OR, —CH(OR)2, —CH(OR)(NR2), —CH(NR2)2, (C1-C6) alkyl;R=each independently —H, —C1-C6 alkyl, -aryl, —CH2Aryl;X1═—H, —Cl, —Br, —I, X2═—Cl, —Br, —I, —N(R2)2, —OSO2RX3=each independently —H, —OR, —NR2, —Cl, —Br, —I, —SR, —SO2R, —SO3R, —SR2+;and X4═—Cl, —Br, —I, OTs, +NR3, -pyridium, and |
