178371-86-3

Upstream product

• 5291-77-0 1-benzyl-2-pyrrolidone 
• 100-39-0 benzyl bromide 
• 81976-70-7 3-benzyl-2-pyrrolidinone 

Downstream Products

• 178371-87-4 1-benzyl-3-(phenylmethyl)-3-(2-(t-butyldimethylsilyloxy)ethyl)-2-oxopyrrolidine 

Relevant academic research and scientific papers

Synthesis of quaternary α-perfluoroalkyl lactams via electrophilic perfluoroalkylation

Efficient protocols enabling the rapid installation of trifluoromethyl, as well as further functionalized fluoroalkyl groups by an electrophilic perfluoroalkylation of lactam-derived ketene silyl amides (KSAs) using hypervalent iodine reagents 1 and 2 have been developed.

Palladium(II)-Catalyzed Allylic C H Oxidation of Hindered Substrates Featuring Tunable Selectivity Over Extent of Oxidation

The use of Oxone and a palladium(II) catalyst enables the efficient allylic C H oxidation of sterically hindered α-quaternary lactams which are unreactive under known conditions for similar transformations. This simple, safe, and effective system for C H activation allows for unusual tunable selectivity between a two-electron oxidation to the allylic acetates and a four-electron oxidation to the corresponding enals, with the dominant product depending on the presence or absence of water. The versatile synthetic utility of both the allylic acetate and enal products accessible through this methodology is also demonstrated.

PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS

Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected fr

SUBSTITUTED 4-(1H-BENZIMIDAZOL-2-YL)[1,4]DIAZEPANES USEFUL FOR THE TREATMENT ALLERGIC DISEASES

The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4] diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

A kinetic EPR study of the dissociation of 1-carbamoyl-1-methylcyclohexa-2,5-dienyl radicals: Release of aminoacyl radicals and their cyclisation

Hydrogen atom abstraction from 1-carbamoyl-1-methylcyclohexa-2,5-dienes generated the corresponding delocalised 1-carbamoyl-1-methylcyclohexa-2,5-dienyl radicals at temperatures below ca. 300 K. At higher temperatures suitably substituted examples dissociated to produce toluene and aminoacyl (carbamoyl) radicals. Both types of intermediate were detected and characterised in solution by EPR spectroscopy. From measurements of the concentrations of the initial and released radicals, rate constants and Arrhenius parameters for dissociation of 1-carbamoyl-1-methylcyclohexa-2,5-dienyl radicals were determined. It was found that dissociation to give a secondary aminoacyl radical [·C(O)N(R)CH2Ph] took place with a rate constant in the range 50 to 90 s-1 at 300 K. The alternative dissociation of the 1-carbamoyl-1-methylcyclohexa-2,5-dienyl radicals to release methyl radicals and an aromatic amide was much slower and did not compete. Analogous dissociations giving primary aminoacyl radicals [·C(O)NHR] were significantly slower. Aminoacyl radicals with allyl, butenyl or similar side chains underwent cyclisation and, in the case of the 1,2,2-trimethylbut-3-enyl derivative, cyclisation was faster than dissociation of the parent cyclohexadienyl radical throughout the accessible temperature range. Semi-empirical AM1 and ab initio DFT computations indicated the decarbonylations of the aminoacyl radicals did not compete with cyclisations.

Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases

The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease

The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases

The present invention relates to novel substituted piperidine derivatives of formula (1), stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

Substituted piperidines useful for the treatment of allergic diseases

The present invention relates to novel substituted piperidine derivatives of the formula STR1stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic diseases including: seasonal rhinitis, allergic rhinitis, and sinusitis.

Anticonvulsant and anxiolytic lactam and thiolactam derivatives

This invention relates to lactam and thiolactam derivatives having useful anticonvulsant and anxiolytic activity, pharmaceutical compositions containing these compounds and therapeutic applications using such compositions.