14-07-2016 дата публикации
Номер: US20160200672A1
Принадлежит:
A process for the preparation of a compound of formula (I): 2. A process according to claim 1 , wherein the coupling reaction is carried out in the presence of a secondary amine.3. A process according to claim 2 , wherein Ris pent-3-yl.9. A process according to claim 1 , wherein the coupling reaction is followed by a mineral acid quenching with hydrofluoric acid claim 1 , hydrochloric acid claim 1 , boric acid claim 1 , acetic acid claim 1 , formic acid claim 1 , nitric acid claim 1 , phosphoric acid or sulfuric acid.10. A process according to claim 1 , wherein the coupling reaction is followed by a hydrochloric acid quenching.11. A process according to claim 1 , wherein a nonprotic solvent is present.12. A process according to claim 11 , wherein the nonprotic solvent is tetrahydrofuran.13. A process according to claim 11 , wherein the alkylating agent is 1-halo-CHRor a sulfonate ester of RCH—OH wherein Ris defined in .14. A process according to claim 1 , wherein the alkylating agent is 1-halo-2-ethylbutane.15. A process according to claim 1 , wherein the alkylating agent is 2-ethyl-1-butanol.16. A process according to claim 1 , wherein the alkylating agent is 1-bromo-2-ethylbutane.17. A process according to claim 1 , wherein the Grignard reagent is a (C-C)alkyl-magnesium-halide claim 1 , phenyl-magnesium-halide claim 1 , heteroaryl-magnesium-halide or a (C-C)cycloakyl-magnesium-halide.18. A process according to claim 1 , wherein the Grignard reagent is methylmagnesiumchloride.19. A process according to claim 2 , wherein the secondary amine is diethylamine or diisopropylamine.20. A process according to claim 2 , wherein the secondary amine is diethylamine.21. A process according to claim 2 , wherein the secondary amine is in a catalytic amount.22. A process according to claim 2 , wherein 0.01 to 0.5 equivalents of the secondary amine is used.23. A process according to claim 2 , wherein the process is continuous.24. A process according to claim 8 , wherein the ...
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