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US 2003/0119873 A1Published application
Methods for preparing sodium-hydrogen exchanger type-1 inhibitors
AssigneePfizer Inc.
InventorsFrank R. Busch, Gregory J. Withbroe
Life of this patent
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Abstract
This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ 1 and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.
Claims13
A method of preparing a compound of formula I′
- 12
- comprising:
- combining a mixture of acetonitrile and a compound of formula IX′
- 13
- with thionyl chloride to form a mixture comprising a compound of formula X′;
- 14
- evaporating excess thionyl chloride from said mixture to form an evaporated mixture;
- and
- combining said evaporated mixture with guanidine to form a compound of formula I′, wherein R1 is methylsulfonyl or hydrogen, R2 is hydrogen or a halogen, R3 is hydrogen, R4 is hydrogen or a halogen, or R3 and R4, together with the carbon atoms to which they are attached, form a six member fully unsaturated ring having one hetero atom that is nitrogen.
6 more elements
A method of preparing a pharmaceutical composition comprising:
- combining a mixture of acetonitrile and a compound of formula IX′
- 15
- with thionyl chloride to form a mixture comprising a compound of formula X′;
- 16
- evaporating excess thionyl chloride from said mixture to form an evaporated mixture;
- combining said evaporated mixture with guanidine to form a final mixture comprising a compound of formula I′
- 17
- isolating said compound of formula I′ from said final mixture;
- and
- combining said compound of formula I′, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable vehicle, diluent or carrier, wherein R1 is methylsulfonyl or hydrogen, R2 is hydrogen or a halogen, R3 is hydrogen, R4 is hydrogen or a halogen, or R3 and R4 , together with the carbon atoms to which they are attached, form a six member fully unsaturated ring having one hetero atom that is nitrogen.
7 more elements
Dependencies are inferred from the claim text.