76403-12-8

Upstream product

• 103-82-2 phenylacetic acid 
• 14815-73-7 methyl allylphenylacetate 

Downstream Products

• 104787-93-1 N-(S)-sec-butyl-2-phenyl-4-pentenamine 
• 104787-97-5 N-(-)-menthyl-2-phenyl-4-pentenamide 
• 76403-13-9 2-Phenyl-pent-4-enoyl azide 
• 34522-48-0 2-phenyl-4-pentenenamide 
• 1026452-26-5 allylphenylketene 
• 1252553-52-8 C₂₂H₂₁ClO₂ 
• 169466-55-1 (S)-2-phenylpent-4-enoic acid, N-methyl amide 
• 14815-78-2 2-phenyl-pent-4-enoic acid benzyl ester 
• 1458027-16-1 N-methyl-N,2-diphenylpent-4-enamide 

Relevant academic research and scientific papers

Isothiourea-Catalyzed Acylative Kinetic Resolution of Tertiary α-Hydroxy Esters

A highly enantioselective isothiourea-catalyzed acylative kinetic resolution (KR) of acyclic tertiary alcohols has been developed. Selectivity factors of up to 200 were achieved for the KR of tertiary alcohols bearing an adjacent ester substituent, with both reaction conversion and enantioselectivity found to be sensitive to the steric and electronic environment at the stereogenic tertiary carbinol centre. For more sterically congested alcohols, the use of a recently-developed isoselenourea catalyst was optimal, with equivalent enantioselectivity but higher conversion achieved in comparison to the isothiourea HyperBTM. Diastereomeric acylation transition state models are proposed to rationalize the origins of enantiodiscrimination in this process. This KR procedure was also translated to a continuous-flow process using a polymer-supported variant of the catalyst.

N-PHENYL-LACTAM DERIVATIVES CAPABLE OF STIMULATING NEUROGENESIS AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

The present invention relates to compounds of the general formula I wherein Het, R1, R2, W and X are as defined herein. Compounds of formula I are useful for treating neuropsychiatric disorders.

N-PHENYL-LACTAM DERIVATIVES CAPABLE OF STIMULATING NEUROGENESIS AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

The present invention relates to compounds of the general formula I wherein Het is oxazole-5-yl, pyridin-4-yl, or pyrazol-4-yl; R1/ R2 are, independently from each other, hydrogen, lower alkyl, lower alkoxy, or halogen; W is -CH2- or -CH2CH2-; X is CR3R4 or NR5; R3 is hydrogen or lower alkyl; R4 is -(CH2)n-phenyl, optionally substituted by halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or lower alkyl; R5 is CHR-phenyl or CH2CHR-phenyl, optionally substituted by halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or lower alkyl, or is CHR-pyridin-2, 3 or 4 -yl; R is hydrogen or lower alkyl; n is 0 or 1; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomer thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine.

Room temperature hydroamination of N-alkenyl ureas catalyzed by a gold(I) N-heterocyclic carbene complex

Treatment of an N-4-pentenyl or N-5-hexenyl urea with a catalytic 1:1 mixture of a gold(I) N,N-diaryl imidazol-2-ylidine complex and AgOTf at or near room temperature leads to intramolecular exo-hydroamination to form the corresponding nitrogen heterocycle in excellent yield.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes

(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2 ,3-dihydrobenzthiophene-3,4′-piperidin-1′yl)]butane S-oxide (3) has been identified as a potent CCR5 antagonist lead structure having an IC50 = 35 nM. Herein, we describe the structure-activity relationship studies directed toward the requirement for and optimization of the C-2 phenyl fragment. The phenyl was found to be important for CCR5 antagonism and substitution was limited to small moieties at the 3-position (13 and 16: X = H, 3-F, 3-Cl, 3-Me).

An Efficient and General Synthesis of 5-Substituted Pyrrolidinones

2-Pyrrolidinone derivatives are widespread materials of considerable laboratory and commercial importance.In spite of this, there is no generally useful synthesis of either symmetrically or unsymmetrically 5,5-disubstituted derivatives.This is particularl