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US 2008/0167488 A1Published application
Process for the Preparation of Geminal ((Difluorocycloalkyl)Methyl) Amines
AssigneeAstraZeneca AB
InventorMaxime Tremblay
Life of this patent
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Abstract
The present invention relates to a process of preparing a compound of formula II, wherein R1, n, m and p are defined in the specification.
Claims18
A process of making a compound comprising:
- a first step of reacting a compound of formula I with (dialkylamino)sulfur trifluoride to form a first compound,
- wherein R1 is selected from hydrogen, C1-6alkyl, C2-6alkenyl, halogenated C1-6alkyl, C1-6alkoxy, —OH, and amino;
- and
- n, m, and p are independently selected from 0, 1 and 2.
1 more element
A process of making a compound comprising reacting a compound of formula V with a with a reducing agent,
- wherein R1 is selected from hydrogen, C1-6alkyl, C2-6alkenyl, halogenated C1-6alkyl, C1-6alkoxy, —OH, and amino;
- and
- n, m, and p are independently selected from 0, 1 and 2.
A process of making a compound of formula II including the steps of:
- a) reacting a compound of formula IV with a tosylmethyl isocyanide at a temperature between −25° C. and 150° C. to form a compound of formula III,
- b) reacting a compound of formula III with water and a hydrolysis catalyst to form a compound of formula I,
- c) reacting a compound of formula I with (dialkylamino)sulfur trifluoride to form a compound of formula V,
- d) reacting a compound of formula V with a with a reducing agent to form the compound of formula II,
- wherein R1 is selected from hydrogen, C1-6alkyl, C2-6alkenyl, halogenated C1-6alkyl, C1-6alkoxy, —OH, and amino;
- and
- n, m, and p are independently selected from 0, 1 and 2.
4 more elements
Dependencies are inferred from the claim text.