2 - substituted-5-oxo-3-pyrazoline Jolly Dean-carboxylate in the manufacture and use

摘要

Preparation of 2-substituted-5-oxo-3-carboxylate Fira Jolie Dean compounds of formula (I) method is disclosed. This is the formula R ¹ OC (O) C (H) (X) C (R ^2a ) (R ^2b ) C (O ) Y (i.e. formula II) (where, X and Y is a leaving group and L, R ¹ , R ^2a and R ^2b is acid derivatives of the same as) defined in the description formula LNHNH ₂ (i.e., includes contacting under a substituted hydrazine and an appropriate acid scavenger, and a solvent in the presence of the formula III). X ¹ , R ⁶ , R ⁷ , R ^8a , R ^8b , R ⁹ and n is also disclosed a process for producing a compound of formula IV as defined in the specification. R ¹ , R ^2a , R ^2b , R ³ , R ⁴ and R ⁵ as defined in the specification; X is Cl, Br or I; Y is F, Cl, Br or I; The stage R ^2a and R ^2b are each H, if X and Y are each Cl R ¹ is not a benzyl R ^2a and R ^2b are each phenyl, if X and Y are each Cl, R ¹ is other than methyl or ethyl, based on weight of the compound of formula II also disclosed is a composition comprising from about 20 to 99%. Formula R ¹ OC (O) C (H) (X) C (R ^2a ) (R ^2b ) CO ₂ H (i.e. formula VI) and from the compound (here the R ^2a and R ^2b is H, X is Br, R ¹ is methyl), a crystalline composition comprising at least about 90% by weight is also disclosed.