Abstract:
This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
Abstract:
A process is described for preparing isoxazoles of the formula I where the substituents are as defined below: R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; which comprises preparing an intermediate of the formula VI where R1, R3, R4 and R5 are as defined above, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of the formula I. Also novel intermediates for preparing the compounds of the formula I and novel processes for preparing the intermediates are described.
Abstract:
A process is described for preparing isoxazoles of the formula I where the substituents are as defined below: R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; which comprises preparing an intermediate of the formula VI where R1, R3, R4 and R5 are as defined above, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of the formula I. Also novel intermediates for preparing the compounds of the formula I and novel processes for preparing the intermediates are described.
Abstract:
A method for efficiently extracting a reaction product containing a target aromatic fluorine compound formed by the halogen exchange reaction of an aromatic chlorine compound with a fluorinating agent quickly from the reaction vessel without suffering part of the reaction product to remain as a residue inside the reaction vessel is disclosed. Specifically, the reaction product is extracted from the reactor subsequently to the halogen exchange reaction at a temperature in the range of 20-250° C. By this method, the reaction product formed in consequence of the halogen exchange reaction can be efficiently extracted quickly from the reaction vessel, and that without suffering occurrence of a residue of the reaction product.
Abstract:
A process for selective, direct oxidation of amine or amine hydrochloride mpounds is described. It uses mixed oxidizing agents of monopersulfate and ozone.
Abstract:
2-NITRO-4,6-DICHLORO-5-METHYLPHENOL IS PREPARED BY THE SULFONATION OF 4-CHLORO-5-METHYLPHENOL TO FORM 2-SULFO-4-CHLORO-5-METHYLPHENOL WHICH IS CHLORINATED TO 2-SULFO-4,6-DICHLORO-5-METHYLPHENOL WHICH IS IN TURN REACTED WITH NITRIC ACID TO FORM THE DESIRED PRODUCT. The sulfonation is carried out with concentrated sulfuric acid at elevated temperatures to form 2-sulfo-4-chloro-5-methylphenol. Thereafter the reaction mixture is diluted with water to a sulfuric acid content of 20-30%. The resulting 2-sulfo-4-chloro-5-methylphenol is chlorinated with chlorine at elevated temperature and normal or elevated pressures to form 2-sulfo-4,6-dichloro-5-methylphenol which is then reacted with nitric acid.
Abstract:
A method for preparing 2-nitro-4, 6-dichloro-5-methylphenol and the corresponding 2-amino compound comprising sulfonating 4chloro-5-methylphenol with a sulfuric anhydride complex in a halogenated hydrocarbon solvent, chlorinating the thus obtained 2-sulfo-4-chloro-5-methylphenol, replacing the sulfonic group of the resulting 2-sulfo-4, 6-dichloro-5-methylphenol with a nitro group and, when the 2-amino compound is required, reducing the nitro group to the amino group is disclosed. The product is useful as an intermediate in preparing a cyan coupler.