187523-36-0

Upstream product

• 206194-00-5 5-chloro-α-fluoro-2-methoxy-α-[2-nitro-4-(trifluoromethyl)-phenyl]benzeneacetic acid,methyl ester 
• 385764-29-4 (+)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-6-(trifluoromethyl)-2H-indol-2-one 
• 343-69-1 6-(Trifluoromethyl)-1H-indol-2,3-dione 
• 26939-01-5 5-chloro-2-methoxyphenylacetic acid,methyl ester 
• 635305-45-2 2-(5-chloro-2-(methoxy)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 183720-28-7 3-(5-Chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-2H-indol-2-one 
• 89694-48-4 5-chloro-2-methoxyphenyl boronic acid 
• 183720-15-2 3-(5-Chloro-2-methoxyphenyl)-1,3-dihydro-3-hydroxy-6-(trifluoromethyl)-2H-indol-2-one 
• 183720-52-7 methyl 2-(5-chloro-2-methoxyphenyl)-2-(2-nitro-4-(trifluoromethyl)phenyl)acetate 
• 367-86-2 1-fluoro-2-nitro-4-trifluoromethyl-benzene 
• 206194-02-7 (S)-(-)-5-Chloro-2-methoxy-α-fluoro-α-[2-nitro-4-(trifluoromethyl)phenyl]benzeneacetic acid 
• 159684-36-3 (2-tert-Butoxycarbonylamino-4-trifluoromethyl-phenyl)-oxo-acetic acid ethyl ester 
• 109134-07-8 t-butyl<3-(trifluoromethyl)phenyl>-carbamate 
• 98-16-8 3-trifluoromethylaniline 

Relevant academic research and scientific papers

Novel synthesis method for Flindokalner raceme

The invention discloses a novel synthesis method for a Flindokalner raceme. The method comprises the steps: subjecting 3-fluoro-3-(2,2,2-trifluoro-1,1-dihydroxyethyl)-6(trifluoromethyl)2H-indol-2-one, which serves as a raw material, to a bromation reactio

Ionic Liquid-Mediated Hydrofluorination of o-Azaxylylenes Derived from 3-Bromooxindoles

The hydrofluorination reaction of 3-bromooxindole using mild HF reagents in an ionic liquid is described. This transformation can operate at room temperature to give a series of 3-substituted 3-fluorooxindole derivatives including racemic BMS 204352 (MaxiPost). The mechanistic study about interactions between HF and 3-butyl-1-methylimidazolium tetrafluoroborate [bmim][BF4] is also discussed on the basis of energy calculations.

Highly enantioselective fluorination of unprotected 3-substituted oxindoles: One-step synthesis of BMS 204352 (MaxiPost)

The catalytic enantioselective fluorination of N-H-free 3-substituted oxindoles was accomplished by a Sc(III)/N,N′-dioxide complex. Under mild reaction conditions, a series of 3-aryl- and 3-alkyl-3-fluoro-2-oxindoles were obtained in excellent yields (up to 98%) and enantioselectivities (up to 99% ee) by using N-fluorobisbenzenesulfonimide (NFSI) as the fluorination agent. MaxiPost was synthesized efficiently in 81% yield with 96% ee.

Highly enantioselective fluorination of unprotected 3-substituted oxindoles: One-step synthesis of BMS 204352 (MaxiPost)

The catalytic enantioselective fluorination of N-H-free 3-substituted oxindoles was accomplished by a Sc(III)/N,N′-dioxide complex. Under mild reaction conditions, a series of 3-aryl- and 3-alkyl-3-fluoro-2-oxindoles were obtained in excellent yields (up to 98%) and enantioselectivities (up to 99% ee) by using N-fluorobisbenzenesulfonimide (NFSI) as the fluorination agent. MaxiPost was synthesized efficiently in 81% yield with 96% ee.

Catalytic enantioselective fluorination of oxindoles

We have developed a highly efficient catalytic enantioselective fluorination of oxindole derivatives. In the presence of a catalytic amount of chiral Pd complex 2 (2.5 mol %), various substrates, including aryl- and alkyl-substituted oxindoles, were fluor

PREPARATION OF 3-FLUORO OXINDOLE DERIVATIVES

The present invention relates to novel itermediates of formula (1) wherein the wavy bond ( SIMILAR SIMILAR ) represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt;

Carbohydrate prodrugs of fluorooxindoles

The present invention provides novel prodrug derivatives of fluorooxindoles having the general Formula I wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer, and R1, R2, R3, R4

Enantioselective synthesis of BMS-204352 (MaxiPost) using N-fluoroammonium salts of cinchona alkaloids (F-CA-BF4).

The enantioselective synthesis of a potent Maxi-K potassium channel opener (BMS-204352) mediated by N-fluoroammonium salts of cinchona alkaloids is described. Two synthetic pathways were evaluated. An ee as high as 88% was achieved (>99% after a single re

Use of 3-substituted oxindole derivatives as kcnq potassium channel modulators

The present invention relates to a novel method of treating of pain or anxiety, using compounds that modulate KCNQ potassium channels and currents.

Enantioselective fluorination mediated by N-fluoroammonium salts of cinchona alkaloids: First enantioselective synthesis of BMS-204352 (maxipost)

We have employed a cinchona alkaloid/Select-fluor-mediated enantioselective fluorination of the oxindole 2 to achieve the first enantioslective synthesis of BMS-204352 (MaxiPost, S-1), an effective opener of maxi-K channels. Fluorination occurred to produce S-1 with 84% ee using the bis-cinchona alkaloid (DHQ)2AQN. Recrystallization produced enantiomerically pure (>99% ee) product. Quinidine-mediated fluorination of 2 gave the (R)-antipode of 1 with 68% ee.