37742-99-7

Upstream product

• 27064-94-4 4,4'-difluorobenzhydryl chloride 
• 506-64-9 silver(I) cyanide 
• 459-22-3 4-fluorophenylacetonitrile 
• 7727-37-9 nitrogen 
• 7677-24-9 trimethylsilyl cyanide 
• 365-24-2 4,4'-difluorobenzhydryl alcohol 
• 460-00-4 1-Bromo-4-fluorobenzene 
• 1765-93-1 4-fluoroboronic acid 
• 151-50-8 potassium cyanide 
• 462-06-6 fluorobenzene 

Downstream Products

• 131912-07-7 α,α-bis(4-fluorophenyl)-1-[(4-methylphenyl)sulfonyl]-3-pyrrolidineacetonitrile 
• 111952-40-0 Bis-(4-fluoro-phenyl)-[1-(toluene-4-sulfonyl)-piperidin-3-yl]-acetonitrile 
• 111952-35-3 α,α-bis(4-fluorophenyl)-1-<(4-methylphenyl)sulfonyl>-4-piperidineacetonitrile 
• 131912-10-2 α,α-bis(4-fluorophenyl)-1-[(4-methylphenyl)sulfonyl]-3-piperidinepropanenitrile 
• 98383-56-3 4-fluoro-β-(4-fluorophenyl)benzeneethanamine 
• 939437-24-8 (2-(Bis-(4-fluorophenyl)methyl)-4-hydroxythiazol-5-yl)acetic acid 
• 939437-30-6 2,2-Bis-(4-fluorophenyl)acetamidine 
• 135256-92-7 α,α-bis(4-fluorophenyl)-3-pyrrolidinepropanenitrile 
• 135256-93-8 3-<2-cyano-2,2-bis(4-fluorophenyl)ethyl>-1-pyrrolidinecarboxylic acid phenyl ester 
• 131911-42-7 1-[3-(4-acetyl-2-methoxyphenoxy)propyl]α,α-bis(4-fluorophenyl)-3-pyrrolidinepropanenitrile 
• 111952-36-4 α,α-bis(4-fluorophenyl)-4-piperidineacetonitrile 
• 111951-85-0 {1-[3-(4-Acetyl-2-methoxy-phenoxy)-propyl]-piperidin-4-yl}-bis-(4-fluoro-phenyl)-acetonitrile 
• 566884-12-6 C₁₇H₁₃F₂N 
• 331629-10-8 2,2-bis(4-fluorophenyl)-5-hydroxypentylamine 

Relevant academic research and scientific papers

Different Selectivities in the Insertions into C(sp2)?H Bonds: Benzofulvenes by Dual Gold Catalysis Competition Experiments

An unprecedented, often almost quantitative access to tricyclic aromatic compounds by dual gold catalysis was developed. This synthetic route expands the scope of benzofulvene derivatives through a C(sp2)?H bond insertion in easily available starting materials. The insertion takes place with an exclusive chemoselectivity with respect to the competing aromatic C?H positions. A bidirectional synthesis with two competing ortho-aryl C?H bonds in the selectivity-determining step also shows perfect selectivity; this result is explained by a computational investigation of the two conceivable intermediates. The intramolecular competition of two non-equivalent aryl C?H bonds with a benzylic methyl group also showed perfect selectivity.

I2-Mediated oxidative bicyclization of 4-pentenamines to prolinol carbamates with CO2 incorporating oxyamination of the C=C bond

A metal-free oxyamination reaction of alkenes with ambient CO2 is reported. In the presence of I2 and DBU, CO2 is applied in situ as a protecting group to regulate the nucleophilicity of the amino group and facilitate the bicyclization of 4-pentenamines with high chemoselectivity. Moreover, this reaction provided a feasible approach to prepare prolinol carbamates with good tolerance of functional groups and high efficiency under mild conditions.

Dual gold catalysis: Synthesis of polycyclic compounds via C-H insertion of gold vinylidenes

New and interesting polycyclic compounds have been synthesized from non-conjugated diyne systems by dual gold catalysis. A quaternary carbon center in the backbone and the accompanying Thorpe-Ingold effect enabled the unprecedented insertion of sp3 and sp2 C-H bonds that for the first time were incorporated within the backbone of the diyne system and allowed the construction of complex polycyclic carbon scaffolds inaccessible by previous approaches in which the C-H bonds for the insertion were situated at the other end of the alkyne.

6-azabicyclo[3.2.1]octanes via copper-catalyzed enantioselective alkene carboamination

Bridged bicyclic rings containing nitrogen heterocycles are important motifs in bioactive small organic molecules. An enantioselective copper-catalyzed alkene carboamination reaction that creates bridged heterocycles is reported herein. Two new rings are

Process development and optimization for production of a potassium ion channel blocker, ICA-17043

A scalable process for the manufacture of a potassium ion channel blocker was developed and optimized. Key features of the process include an optimized Grignard reaction, a direct cyanation of the intermediate trityl alcohol derivative, and an improved nitrile hydrolysis protocol, relative to the original acidic hydrolysis conditions, to generate the crude active pharmaceutical ingredient (API) with >95% HPLC purity. The Grignard and the cyanation reactions could be telescoped, resulting in an improved throughput compared to the original four-step process. An effective recrystallization of the API was also developed and the process scaled up to manufacture multiple batches at the pilot scale.

Zn(OTf)2 - Catalyzed direct cyanation of benzylic alcohols - A novel synthesis of α-aryl nitriles

This work demonstrates an efficient method to prepare α-aryl nitriles by direct cyanation of benzylic alcohol with TMSCN in the presence of a catalytic amount of Zn(OTf)2 under heating condition. A variety of benzylic alcohols can be converted into the corresponding α-aryl nitriles in good to excellent yields. 2012 Elsevier Ltd. All rights reserved.

Synthesis of α-aryl nitriles through B(C6F5)3-catalyzed direct cyanation of α-aryl alcohols and thiols

Various α-aryl nitriles have been prepared in excellent yield from the corresponding α-aryl alcohols employing 3 mol % of B(C6F5)3 (1) as Lewis acid catalyst and (CH3)3SiCN (TMSCN) as cyanide source. Cyano transfer from TMSCN to alcohol proceeds within short reaction time at rt. α-Aryl thiols also produce corresponding nitriles in good to excellent yield at reflux condition.

THIAZOLYL- AND PYRIMIDINYL-ACETIC ACIDS AND THEIR USE AS CRTH2 RECEPTOR LIGANDS

[2-[Bis-(4-fluoro-phenyl)methyl]-4-(2-methylpyridin-4-yl)thiazol-5-yl]acetic acid, {4-(2-aminopyridin-4-yl)-2-[bis-(4-fluorophenyl)methyl]thiazol-5-yl}acetic acid, [2-[bis-(4-fluoro-phenyl)-methyl]-4-(3-fluoro-phenyl)-pyrimidin-5-yl]acetic acid, and salts

MELANIN CONCENTRATING HORMONE ANTAGONISTS

A compound represented by the formula wherein Ar1 and Ar2 are each an aromatic group optionally having substituents, P and Q are each a divalent aliphatic hydrocarbon group which optionally contains ether oxygen or ether sulfur in a carbon chain and which

Phenyl-substituted normethadones: Synthesis and pharmacology

Phenyl-substituted normethadone derivatives were synthesized and their affinity (IC50) for opioid receptors was determined by displacement of the specific binding sites of [3H]sufentanyl on rat brain preparations. Substitution resulted in a decrease of affinity in-vitro. These results suggest that normethadone-like compounds may interact with the P subsite of the μ-opioid receptor and that the P subsite has a well-defined cavity shape of stringent dimensions.