132301-89-4

Usage

Uses

(S)-Cloperastine is used in the treatment of chronic non-productive cough. Antitussive.

Upstream product

• 119-56-2 (4-chlorophenyl)phenylmethanol 
• 110-89-4 piperidine 
• 5321-46-0 (4-chlorophenyl)phenylmethyl 2-chloroethyl ether 
• 3703-76-2 Cloperastine 
• 2008-75-5 N-chloroethylpiperidine hydrochloride 
• 123535-85-3 (R)-(4-chlorophenyl)phenylmethanol 
• 17964-15-7 4-trimethylsilanyl-benzhydrol 

Relevant academic research and scientific papers

A simple and cost-effective synthesis of sulfated β-cyclodextrin and its application as chiral mobile phase additive in the separation of cloperastine enantiomers

A simple and cost-effective method for the synthesis of sulfated β-cyclodextrin, one of the most widely used chiral mobile phase additives, using sulfamic acid as a sulfonating agent has been described. The method was optimized, and the synthesized product was characterized by spectroscopic, size-exclusion chromatographic, thermal, and microscopic methods and was compared to the marketed Sigma Aldrich sulfated β-cyclodextrin. β-Cyclodextrin, hydroxypropyl β-cyclodextrin, sulfated β-cyclodextrin (marketed and synthesized) were evaluated as chiral mobile phase additives for the enantiomeric separation of cloperastine, an antitussive agent, using reversed-phase HPLC. Under optimized conditions, a resolution of 3.14 was achieved within 15?min on an achiral Kromasil C8 (150 × 4.6?mm, 5?μm) column, with 5?mM monopotassium phosphate containing 10?mM synthesized sulfated β-cyclodextrin pH 3.0 and 45% methanol?as mobile phase. The method utilizing synthesized sulfated β-cyclodextrin as chiral mobile phase additive was validated as per ICH guidelines and applied for the quantitative determination of cloperastine enantiomers in active pharmaceutical ingredients and pharmaceutical formulations. The selectivity changes imparted by sulfated β-cyclodextrin were proven to be beneficial for chiral separation. For the enantiomeric separation of cloperastine, synthesized sulfated β-cyclodextrin afforded better resolution than marketed sulfated β-cyclodextrin.

A left hand chlorine paipai Si Tingfenoak acid preparation method of the

The invention discloses a preparation method of levo cloperastine fendizoate, which comprises the following steps: carrying out nucleophilic substitution reaction on 4-chlorobenzhydrol and 2-chloroethanol in a benzene organic solvent, so that an intermediate product is obtained; reacting the intermediate product with piperidine, so that racemic cloperastine is obtained; resolving the racemic cloperastine by using a resolving agent in a fatty alcohol solvent, so that levo cloperastine is obtained; and carrying out salt forming reaction on the levo cloperastine and a fendizoic acid, so that levo cloperastine fendizoate is obtained, wherein the resolving agent is an R-substituted dibenzoyl-L-tartaric acid, and R refers to alkyl, alkoxy, -Cl, -F, -Br or -H. In the method provided by the invention, in a fatty alcohol solvent, an R-substituted dibenzoyl-L-tartaric acid is adopted as a resolving agent for carrying out resolving on racemic cloperastine, and the resolving yield is high, so that the obtained levo cloperastine fendizoate has high optical purity, and has a high product yield.

Novel Intermediate of L-Cloperastine and Preparation Method Thereof

The present invention refers to pharmaceutically useful as well as novel intermediates of [...][...] -L (cloperastine) manufacturing method relates to and, more specifically a device with structure of formula 1 L- [...] intermediates manufacturing method of using enzymes relates to. Formula 1 , The, R the C1-C3 copyright 2000. (by machine translation)

Dynamic kinetic resolution of diarylmethanols with an activated lipoprotein lipase

We explored the kinetic resolution of 31 different diarylmethanols with an activated lipoprotein lipase (LPL-D1) which was about 3000-fold more active than its native counterpart in organic solvent. Most of the substrates tested were accepted by LPL-D1 with good to high enantioselectivity in the kinetic resolution. Next, we explored the dynamic kinetic resolutions (DKRs) of these substrates (24 out of 31) using LPL-D1 and a ruthenium-based racemization catalyst in combination, which provided satisfactory yields (71-96%) and high enantiopurities (90-99% ee). As an illustrative example for the synthetic applications of the DKR procedure, we synthesized L-cloperastine, an antitussive drug, from phenyl-(p-trimethylsilylphenyl)methanol via DKR. (Chemical Equation Presented).