PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES, INTERMEDIATE COMPOUNDS AND SYNTHESIS Russian patent published in 2010 - IPC C07D487/04 C07D211/56 

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