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US 6,635,767 B2Granted
Synthesis of heteroarylamine intermediate compounds
AssigneeBoehringer Ingelheim Pharmaceuticals, Inc.
InventorsJinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
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Abstract
Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
Claims6
A compound of the formula:
- Xa, is Br attached via the 5 ring position;
- Xb is chosen from Br, Cl and I;
- and
- W is CR3 or N, wherein R3 is chosen from hydrogen, C1-5alkyl, C1-5alkoxy and arylC0-5alkyl.
1 more element
A process of making a Grignard compound of the formula(F):
- said process comprising:
- reacting a compound of the formula(C)
- with a magnesium reagent of the formula R—MgXb;
- said reaction taking place in a suitable aprotic solvent at −78° C. to RT, for a reaction time of ½ hour to 2 hours, producing the Grignard compound of the formula(F);
- and wherein
- Xa is Br attached via the 5 ring position;
- Xb is chosen from Br, Cl and I;
- Xc is I;
- W is CR3 or N, wherein R3 is chosen from hydrogen, C1-5alkyl, C1-5alkoxy and arylC0-5alkyl;
- and
- R is chosen from aryl, C1-6alkyl and C5-7cycloalkyl.
8 more elements
Dependencies are inferred from the claim text.