Production of pyrrolopyrimidines and intermediates therefor

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) C07D 239/46 (2006.01) C07D 239/48 (2006.01) C07D 239/50 (2006.01)

Patent

CA 2018875

There is provided an improved process for producing novel compounds represented by the general formula: (see formula I) wherein the ring A represents a pyrrole ring which may be hydrogenated; X represents an amino, hydroxyl or mercapto group; R1, R2 and R3, each, being the same as or different from the other, represents hydrogen or an alkyl, alkenyl or alkynyl group which may be substituted; R4 represents OR5 wherein R5 represents hydrogen or a hydrocarbon group which may be substituted or NHCH(COOR6)CH2CH2COOR7 wherein R6 and R7 each represents hydrogen or a hydrocarbon group which may be substituted; and n represents an integer of 1 to 4, or a salt thereof from compounds represented by the general formula: (see formula II) wherein X, R1, R2, R3, R4 and n are the same as defined above; Y1 and Y2 each represents oxygen or sulfur atom; R8 and R9 each, being the same as or different from the other, represents a hydrocarbon group which may be substituted, or salts thereof by an intramolecular ring closure reaction to form a pyrrolo-pyrimidine ring and, if necessary, reducing pyrrole ring thus formed to a pyrroline ring. The compounds are useful as antitumor agents.

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