123803-29-2

Upstream product

• 6216-63-3 N-Cbz-Prolinol 
• 124-63-0 methanesulfonyl chloride 
• 1148-11-4 N-Benzyloxycarbonyl-L-proline 
• 501-53-1 benzyl chloroformate 
• 147-85-3 L-proline 
• 23356-96-9 (S)-1-Pyrrolidin-2-yl-methanol 

Downstream Products

• 172885-53-9 (S)-2-iodomethyl-pyrrolidine-1-carboxylic acid benzyl ester 
• 72500-25-5 (S)-benzyl 2-(cyanomethyl)pyrrolidine-1-carboxylate 
• 199473-04-6 (S)-N-Cbz-2-(2-methoxyphenoxymethyl)pyrrolidine 
• 1316160-32-3 (S)-N-((1-(benzyloxycarbonyl)pyrrolidin-2-yl)methyl)-N,N-dimethylethanaminium bromide 
• 1316160-33-4 (S)-N-((1-(benzyloxycarbonyl)pyrrolidin-2-yl)methyl)-N,N-dimethylpropan-1-aminium bromide 
• 1316160-36-7 (S)-N-((1-(benzyloxycarbonyl)pyrrolidin-2-yl)methyl)-N,N-dimethylbutan-1-aminium bromide 
• 1316160-39-0 (S)-N-((1-(benzyloxycarbonyl)pyrrolidin-2-yl)methyl)-N,N-dimethyloctan-1-aminium bromide 
• 1316160-41-4 (S)-1-(1-(benzyloxycarbonyl)pyrrolidin-2-yl)-N,N,N-trimethylmethanaminium bromide 
• 101250-72-0 (S)-2-Acetylsulfanylmethyl-pyrrolidine-1-carboxylic acid benzyl ester 
• 1355731-10-0 (S)-N,N-dimethyl-2-phenyl-N-(pyrrolidin-2-ylmethyl)ethanaminium bromide 
• 1355731-09-7 (S)-1-cyclopropyl-N,N-dimethyl-N-(pyrrolidin-2-yl-methyl)methanaminium bromide 
• 1355731-07-5 (S)-N-((1-(benzyloxycarbonyl)pyrrolidin-2-yl)methyl)-N,N-dimethyl-2-phenylethanaminium bromide 
• 1355731-05-3 (S)-1-(1-(benzyloxycarbonyl)pyrrolidin-2-yl)-N-(cyclopropylmethyl)-N,N-dimethylmethanaminium bromide 
• 1355731-01-9 (S)-N-((1-(benzyloxycarbonyl)pyrrolidin-2-yl)methyl)-4-cyano-N,N-dimethylbutan-1-aminium bromide 

Relevant academic research and scientific papers

Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists

Some unichiral analogues of 2R,2′S-2-(1′-methyl-2′-pyrrolidinyl)-7-hydroxy-1,4-benzodioxane, a potent and selective α4β2-nAChR partial agonist, were designed by opening dioxane and replacing hydroxyl carbon with nitrogen. The resulting 3-pyridyl and m-hydroxyphenyl ethers have high α4β2 affinity and good subtype selectivity, which get lost if OH is removed from phenyl or the position of pyridine nitrogen is changed. High α4β2 affinity and selectivity are also attained by meta hydroxylating the 3-pyridyl and the phenyl ethers of (S)-N-methylprolinol and the phenyl ether of (S)-2-azetidinemethanol, known α4β2 agonists, although the interaction mode of the aryloxymethylene substructure cannot be assimilated to that of benzodioxane. Indeed, the α4β2 and α3β4 functional tests well differentiate behaviors that the binding tests homologize: both the 3-hydroxyphenyl and the 5-hydroxy-3-pyridyl ether of N-methylprolinol are α4β2 full agonists, but only the latter is highly α4β2/α3β4 selective, while potent and selective partial α4β2 agonism characterizes the hydroxybenzodioxane derivative and its two opened semirigid analogues. (Figure Presented).

Targeted Covalent Inhibition of Prolyl Oligopeptidase (POP): Discovery of Sulfonylfluoride Peptidomimetics

Prolyl oligopeptidase (POP), a serine protease highly expressed in the brain, has recently emerged as an enticing therapeutic target for the treatment of cognitive and neurodegenerative disorders. However, most reported inhibitors suffer from short durati

Asymmetric Michael additions catalysed by functionalised quaternary alkylammonium ionic liquids

Some functionalised quaternary alkylammonium ionic liquids were synthesised and examined as organocatalysts for asymmetric Michael additions of aldehydes and ketones to nitroolefins. All of them exhibited excellent enantioselectivities (>99% ee) and diast

Chiral pyrrolidine quaternary derivatives as organocatalysts for asymmetric Michael additions

A series of chiral pyrrolidine quaternary derivatives were designed and synthesized. It was found that these derivatives are highly efficient organocatalysts for the asymmetric Michael addition reactions of aldehydes and ketones to nitroolefins with high

Pyrrolidine-based chiral quaternary alkylammonium ionic liquids as organocatalysts for asymmetric Michael additions

A series of chiral pyrrolidine-type quaternary alkylammonium ionic liquids were synthesized and served as efficient catalysts for asymmetric Michael additions of aldehydes and ketones to nitroolefins, and the corresponding adducts were obtained in excelle

Novel cyclic β-aminophosphonate derivatives as efficient organocatalysts for the asymmetric Michael addition reactions of ketones to nitrostyrenes

Three novel catalysts based upon cyclic β-aminophosphonate derivatives 13 were designed to catalyze the asymmetric Michael addition reactions of ketones to β-nitrostyrenes. Among the catalysts that have been prepared in this study, cyclic β-aminophosphonic acid monoethylester 3 showed the highest catalytic ability, giving the corresponding Michael adduct in good yields, high enantioselectivities (up to 92%ee), and high diastereoselectivities (syn:anti up to 95:5).

Synthesis of homoproline analogues containing heterocyclic rings and their activity as organocatalysts for Michael reaction

Two homoproline derivatives containing either the 5-thioxo-1,2,4-oxadiazole or the 2-oxo-1,2,3,5-oxathiodiazole bioisosteric groups, in replacement of the carboxyl group, were synthesized and their catalytic activities in Michael reactions were evaluated.

NOVEL ANTIDIABETIC COMPOUNDS HAVING HYPOLIPIDAEMIC, ANTIHYPERTENSIVE PROPERTIES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

New thiazolidin-2,4-dione derivatives of formula (1) in which A, W, Q, B, D, X, Y, Z, R', k and p are defined as in claim 1; their tautomeric forms, their derivatives, their steroisomers, their polymorphs, their pharmaceutical acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. Methods for their preparation and their use as antidiabetic compounds are claimed.

Sulfone derivatives, process for their production and use thereof

A compound represented by the formula: 1wherein R is a cyclic hydrocarbon group, or the like; W is a bond, or the like; X is a divalent hydrocarbon group, or the like; Y and Z are each independently —N(R6)— or the like; ring A is a nitrogen-containing heterocyclic ring, or the like; R5 and R6 are independently hydrogen atom, a hydrocarbon group, or the like; Z′ is imidoyl group, or the like; a is 0, 1 or 2; and b is 0 or 1, or a salt thereof.

Synthesis and application of ligands for the asymmetric addition of organolithium reagents to imines

Amino acid derived ligands 4d,e are prepared from (S)-valine and (S)-proline respectively, and can be used as chiral ligands during the asymmetric addition of organolithium reagents to N-arylimines. Ligand 4e, which is prepared by two independent routes, is found to induce addition of organolithium reagents to the si-face of the imines, whilst ligand 4d in common with the previously reported catalysts 4a-c induces addition to the re-face of the imines.