Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Reexamination Certificate
2007-08-17
2011-12-13
Moore, Susanna (Department: 1624)
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
C514S259300
Reexamination Certificate
active
08076479
ABSTRACT:
Disclosed is a process for the synthesis of compounds of Formula Iby sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,wherein R1is a linear, branched, or cyclic alkyloxy functional group of the structure (—R2a—OH), R2ais a linear, branched or cyclic alkyl group, R2is a linear, branched or cyclic alkyl group, and R3is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1,with a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.
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Chen Frank Xing
Keertikar Kartik M.
Kuo Shen-Chun
Lee Hong-Chang
Raghavan Ramani R.
Jeanette Henry C.
Moore Susanna
Muthard David A.
Schering Corporation
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