288583-04-0

Basic information

• Product Name: amorolfine
• Synonyms: Morpholine, 4-[(2R)-3-[4-(1,1-dimethylpropyl)phenyl]-2-methylpropyl]-2,6-dimethyl-, (2R,6S)-
• CAS NO: 288583-04-0
• Molecular Formula: C21H35 N O
• Molecular Weight: 317.51
• Mol File: 288583-04-0.mol
• Article Data: 10

Chemical Properties

• Appearance: /
• CAS DataBase Reference: amorolfine(CAS DataBase Reference)
• NIST Chemistry Reference: amorolfine(288583-04-0)
• EPA Substance Registry System: amorolfine(288583-04-0)

Safety Data

• Hazardous Substances Data: 288583-04-0(Hazardous Substances Data)

Upstream product

• 1895-97-2 2-methyl-3-phenylacrylic acid 
• 141-91-3 cis-2,6-dimethylmorpholine 
• 1199-77-5 α-methylcinnamic acid 
• 20753-88-2 meso-((1-hydroxypropan-2-yl)oxy)propan-1-ol 
• 141-91-3 2,6-dimethyl morpholine 
• 67467-96-3 2-methyl-3-(4-(tert-pentyl)phenyl)propanal 
• 75-85-4 tert-Amyl alcohol 
• 74879-98-4 N-(2-methyl-3-phenylpropyl)piperidine 
• 583-59-5 2-Methylcyclohexanol 
• 594-36-5 2-methyl-2-butylchloride 

Relevant articles and documents

Preparation method of amorolfine hydrochloride

The invention relates to the technical field of pharmaceutical preparations. The invention discloses a preparation method of amorolfine hydrochloride. The method comprises the following steps: with 3-(4-tert-amylphenyl)-2-methyl propanol as a raw material, under alkaline condition, performing a reaction on the raw material with methylsulfonyl chloride and performing nucleophilic substitution reaction with cis-2,6-dimethylmorpholine; and finally performing a reaction with hydrogen chloride gas to form the amorolfine hydrochloride, that is, the final product. According to the present invention,the method has advantages of cheap raw material source, easily-controlled process operation, high yield, stable quality, less impurity, significantly-reduced cost compared to other methods, suitability for industrial production, and the like.

Amorolfine hydrochloride preparation method

The invention provides an amorolfine hydrochloride preparation method which specifically comprises the following steps: putting a compound of formula IIa shown in the specification into an organic solvent, further putting an amidation catalyst, carrying out a stirring reaction, further adding cis-2,6-dimethyl morpholine, and carrying out a reaction so as to obtain a compound III; carrying out backflow stirring on the compound III in absolute methanol, adding magnesium chips in batches, and carrying out a reaction so as to obtain a compound IV; carrying out a reaction on the compound IV under the action of a reducing agent, thereby obtaining a compound V. The method is novel in process route, cheap and easy in raw material obtaining, low in cost, simple in process operation, short in production cycle, gentle in reaction condition, high in yield, good in product quality and applicable to industrial production.

PROCESS FOR THE PURIFICATION OF AMOROLFINE HYDROCHLORIDE

The present invention relates to a process for the purification of amorolfine hydrochloride by means of a reversed-phase preparative high performances liquid chromatography (prep-HPLC) said method starting from a crude Amorolfine hydrochloride having purity higher than 90% and containing Bepromoline hydrochloride 5% and Fenpropimorf 3%. The process involves the use of a mobile phase comprising water and an organic solvent under isocratic conditions.