发明名称 PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES, INTERMEDIATE COMPOUNDS AND SYNTHESIS
摘要 FIELD: chemistry. ^ SUBSTANCE: invention relates to versions of a novel method of producing pyrrolo[2,3-d]pyrimidine derivatives of general formula V, which have protein kinase inhibiting properties, including a method of producing novel intermediate compounds. The method of producing compounds of formula V , where X1 is an activating group selected from chlorine, bromine, iodine, R1 is (C1-C6)alkyl; a is an integer from 0 to 4; R2 is hydrogen or (C1-C6)alkyl, involves linking an activated pyrrolopyrimidine compound of formula IIa , where L1 is a leaving group and X is an activating group selected from chlorine, bromine, iodide; with an amine of formula IIIa or its salt, where R1 is (C1-C6)alkyl; a is an integer from 0 to 4; R2 is hydrogen or (C1-C6)alkyl and P is a nitrogen protecting group labile to hydrogenolysis, such as benzyl; in the presence of a base to obtain a compound of formula IVa and subsequent removal from the obtained compound of formula IVa of the activating group X1 and the nitrogen protecting group P through hydrogenolysis in the presence of hydrogen or a hydrogen source and a catalyst in any order. ^ EFFECT: method increases output of the desired product. ^ 26 cl, 8 dwg, 15 ex
申请公布号 RU2384583(C2) 申请公布日期 2010.03.20
申请号 RU20080103279 申请日期 2006.07.17
申请人 PFAJZER PRODAKTS INK. 发明人 RUGGERI SALLI GAT;KHOKINS DZHOEHL MAJKL;MAKOVSKI TEREZA MARGARET;REZERFORD DZHENNIFER LI;URBAN FRANK DZHON
分类号 C07D211/56;C07D487/04 主分类号 C07D211/56
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