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US 8,026,384 B2Granted
Process for the synthesis of alkyl phosphinic acids by initiation of an amine and an amineoxide
AssigneeAstraZeneca AB
InventorsDaniel Finnhult, Roger Sohlberg, Fredrik Stalfors, Carina Svensson, Johanna Wachtmeister, Thomas Wannman
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Abstract
The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.
Claims11
A process for the synthesis of a compound of formula I
- wherein
- R1 is selected from hydrogen;
- C1-C10-alkyl;
- C1-C10-alkoxy;
- fluorine;
- and chlorine;
- R2 is selected from hydroxy;
- fluorine;
- chlorine;
- oxo;
- and C1-C10-alkoxy;
- R3 is selected from hydrogen and C1-C6-alkyl;
- R4 is selected from hydrogen and C(O)R5;
- R5 is selected from C1-C10 alkyl and C1-C10 alkoxy;
- comprising reacting a compound of formula II
- wherein
- R6 is selected from hydrogen;
- C1-C10-alkyl;
- C1-C10-alkoxy;
- fluorine;
- and chlorine;
- R7 is selected from hydroxy;
- fluorine;
- chlorine;
- oxo;
- and C1-C10-alkoxy;
- R8 is selected from hydrogen and C1-C6-alkyl;
- R9 is selected from hydrogen and C(O)R10;
- R10 is selected from C1-C10 alkyl and C1-C10 alkoxy;
- and
- X is iodide or bromide;
- with a compound of formula III
- wherein
- R11 and R12 are each and independently selected from C1-C10 alkyl and Si(R13)3;
- and
- R13 is a C1-C6 alkyl;
- in the presence of an amine and an amineoxide.
34 more elements
Dependencies are inferred from the claim text.