906802-36-6

Usage

Type

Small molecule antagonist

Target Receptor

Calcitonin gene-related peptide (CGRP) receptor

Mechanism of Action

Blocks CGRP activity

Therapeutic Use

Treatment of migraine

Effects

Reduces severity and duration of migraine attacks

Specificity

Potent and selective

Mode of Administration

Oral (likely)

Benefits

Provides relief for migraine sufferers

Clinical Studies

Efficacy demonstrated in trials

Potential

Promising option for migraine treatment

Upstream product

• 121282-70-0 (+/-)-trans-1-hydroxy-2-tert-butoxycarbonylamino-cyclohexane 
• 7417-21-2 2-(3,4-dimethoxyphenyl)ethyl alcohol 
• 14189-99-2 (R)-(+)-2-acetoxysuccinic anhydride 
• 931-15-7 (1R,2R)-2-aminocyclohexanol 
• 134108-76-2 (1R,2R)-2-hydroxycyclohexylcarbamic acid benzyl ester 
• 867152-08-7 2-(3,4-dimethoxyphenyl)ethyl 2,2,2-trichloroethanimidate 
• 917979-65-8 (3R)-1-((1R,2R)-2-hydroxycyclohex-1-yl)-2,5-dioxopyrrolidin-3-yl acetate 

Downstream Products

• 794466-70-9 (3R)-1-{(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl}pyrrolidin-3-ol 
• 748810-28-8 Vernakalant hydrochloride 
• 795282-03-0 C₂₂H₃₃NO₅ 
• 1360728-87-5 (3R)-1-(2-(3,4-dimethoxyphenethoxy)cyclohexyl)pyrrolidin-3-ol 

Relevant academic research and scientific papers

Purification method of vernakalant hydrochloride

The invention discloses a purification method of vernakalant hydrochloride. The method comprises the steps of preparation of a vernakalant hydrochloride crude product and purification through the process of alkalinization, nonpolar solvent extraction, acidification and mixed solvent pulping, and thus a qualified product is obtained. The preparation method is simple in operation, mild in condition and easy for industrialized production, and the purity of the product reaches 99.9 percent, and the total impurity and single impurity are both less than 0.1 percent, so that the quality requirements for preparing medicine can be reached, and at the same time, the usage of heavy metal is avoided, and the development of injection forms is facilitated.

Radical-mediated dehydrative preparation of cyclic imides using (NH4)2S2O8-DMSO: Application to the synthesis of vernakalant

Ammonium persulfate-dimethyl sulfoxide (APS-DMSO) has been developed as an efficient and new dehydrating reagent for a convenient one-pot process for the synthesis of miscellaneous cyclic imides in high yields starting from readily available primary amines and cyclic anhydrides. A plausible radical mechanism involving DMSO has been proposed. The application of this facile one-pot imide forming process has been demonstrated for a practical synthesis of vernakalant.

SYNTHETIC PROCESSES FOR THE PREPARATION OF AMINOCYCLOHEXYL ETHER COMPOUNDS

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II) or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

SYNTHETIC PROCESS FOR AMINOCYCLOHEXYL ETHER COMPOUNDS

Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.