1255208-74-2

Upstream product

• 34578-26-2 Boc-L-Ser(Bzl)-Gly-OEt 
• 23680-31-1 BOC-O-benzyl-L-serine 
• 5680-79-5 glycine ethyl ester hydrochloride 
• 70669-05-5 N-(tert-butoxycarbonyl)-O-benzyl-L-seryl-glycine methyl ester 
• 4530-20-5 BOC-glycine 
• 1361215-50-0 methyl O-benzyl-L-serylglycinate trifluoroacetate 

Downstream Products

• 1361222-69-6 1,1,1-trifluoro-2-(4-((2S)-2-(((1-methylethyl)amino)methyl)-4-(thiophen-2-ylsulfonyl)-1-piperazinyl)phenyl)-2-propanol 
• 1361223-36-0 1,1,1-trifluoro-2-(4-((2S)-2-((((3-methyl-3-oxetanyl)methyl)amino)methyl)-4-(thiophen-2-ylsulfonyl)-1-piperazinyl)phenyl)-2-propanol 
• 1361223-23-5 2-(4-((2S)-2-((cyclobutylamino)methyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-1,1,1-trifluoro-2-propanol 
• 1450620-66-2 1,1,1-trifluoro-2-(4-((2R)-2-(((1-methylethyl)sulfanyl)methyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-2-propanol 
• 1450620-67-3 (2R)-1,1,1-trifluoro-2-(4-((2R)-2-(((1-methylethyl)sulfonyl)methyl)-4-(thiophen-2-ylsulfonyl)-1-piperazinyl)phenyl)-2-propanol 
• 1450620-68-4 (2S)-1,1,1-trifluoro-2-(4-((2R)-2-(((1-methylethyl)sulfonyl)methyl)-4-(thiophen-2-ylsulfonyl)-1-piperazinyl)phenyl)-2-propanol 
• 1450620-65-1 1,1,1-trifluoro-2-(4-((2R)-2-(((1-methylethyl)sulfonyl)methyl)-4-(thiophen-2-ylsulfonyl)-1-piperazinyl)phenyl)-2-propanol 
• 1361215-52-2 (3R)-3-((benzyloxy)methyl)-1-(2-thiophenylsulfonyl)piperazine 
• 1361215-53-3 2-(4-((2R)-2-((benzyloxy)methyl)-4-(thiophen-2-ylsulfonyl)-1-piperazinyl)phenyl)-1,1,1-trifluoro-2-propanol 
• 1361215-54-4 1,1,1-trifluoro-2-(4-((2R)-2-(hydroxymethyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-2-propanol 
• 1361215-49-7 ((2R)-4-(2-thiophenylsulfonyl)-1-(4-(2,2,2-trifluoro-1-hydroxy-1-methylethyl)-phenyl)-2-piperazinyl)methyl methanesulfonate 

Relevant academic research and scientific papers

Interfacial supramolecular biomimetic epoxidation catalysed by cyclic dipeptides

We synthesised a library of cis- and trans-cyclic dipeptides and evaluated their efficacy as catalysts in the asymmetric Weitz-Scheffer epoxidation of trans-chalcone. A thorough investigation relying on structure-activity studies and computational studies provided insights into the mechanism of the process. Our results revealed some structural features required for efficient conversion and for introduction of chirality into the product. The cyclic dipeptide acts as a catalyst by templating a supramolecular arrangement at the aqueous-organic interface required for efficient transformations to occur. Among all cyclic dipeptides investigated, cyclo(Leu-Leu) was the most efficient supramolecular catalyst.

A general method for the facile synthesis of optically active 2-substituted piperazines via functionalized 2,5-diketopiperazines

Upon utilization of some common methods described in the literature for the synthesis of chiral, 2-substituted 2,5-diketopiperazines, extensive racemization was observed. Further investigation showed that heating in the presence of a mild base racemized the chiral center in the product diketopiperazines. A generalized, readily scalable route was sought and, after investigating the effect of base and temperature, conditions were identified that promoted cyclization without erosion of enantiomeric excess. An array of functionalization was tolerated and this procedure serves as a useful and reliable method for the facile synthesis of this important class of compounds.

SULFONYL COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN

The present invention relates to sulfonyl compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

SULFONYLPIPERAZINE DERIVATIVES THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES

The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Stereoselective ring contraction of 2,5-diketopiperazines: An innovative approach to the synthesis of promising bioactive 5-membered scaffolds

Ring contraction of 2,5-diketopiperazines by TRAL-alkylation led us to the stereoselective synthesis of original pyrrolidine-2,4-diones, a novel series of promising molecules with moderate anti-proliferative activity on breast cancer cells.

PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES

Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or -CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, N02, CN, COR4, C(O)OR4, CONR5R6 , NR5R6, S02NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen, (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyl is unsubsituted or substituted with a phenyl; R4 is hydrogen, (C1-6 alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treament of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).