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US 2012/0259115 A1Published application
Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis
AssigneePfizer Inc.
InventorsSally Gut Ruggeri, Joel M. Hawkins, Teresa M. Makowski, Jennifer L. Rutherford, Frank J. Urban
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Abstract
This invention relates to methods and intermediates useful for the synthesis of pyrrolo [2,3-d] pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
Claims19
A method of making a compound of the Formula IVa
- comprising coupling an activated pyrrolopyrimidine compound of the Formula IIa
- wherein L1 is a leaving group and X1 an activating group;
- with an amine of the Formula IIIa, or a salt thereof;
- wherein 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;
- in the presence of a base to afford a coupled product of the Formula IVa.
4 more elements
18-47. (canceled)
Dependencies are inferred from the claim text.