37682-80-7

Upstream product

• 3182-93-2 (L)-phenylalanine ethyl ester hydrochloride 
• 503-38-8 trichloromethyl chloroformate 
• 124-38-9 carbon dioxide 
• 2446-83-5 di-isopropyl azodicarboxylate 
• 3081-24-1 H-Phe-OEt 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 75-44-5 phosgene 

Downstream Products

• 1280167-66-9 (2S)-ethyl 2-((((1-((4,8-bis((3,4-dimethoxybenzyl)amino)-6-((2-hydroxypropyl)amino)-pyrimido[5,4-d]pyrimidin-2-yl)amino)propan-2-yl)oxy)carbonyl)amino)-3-phenylpropanoate 
• 1452185-37-3 ethyl 2-[4-(2-ethoxy-2-oxoethyl)-3,5-dioxo-1,2,4-thiadiazolidin-2-yl]-3-phenylpropanoate 
• 66919-79-7 N,N-Bis-<2-chloraethyl>-carbamoyl-L-phenylalanin-aethylester 

Relevant academic research and scientific papers

Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and in Vivo Studies

Rhodesain is a major cysteine protease of Trypanosoma brucei rhodesiense, a pathogen causing Human African Trypanosomiasis, and a validated drug target. Recently, we reported the development of α-halovinylsulfones as a new class of covalent reversible cysteine protease inhibitors. Here, α-fluorovinylsulfones/-sulfonates were optimized for rhodesain based on molecular modeling approaches. 2d, the most potent and selective inhibitor in the series, shows a single-digit nanomolar affinity and high selectivity toward mammalian cathepsins B and L. Enzymatic dilution assays and MS experiments indicate that 2d is a slow-tight binder (Ki = 3 nM). Furthermore, the nonfluorinated 2d-(H) shows favorable metabolism and biodistribution by accumulation in mice brain tissue after intraperitoneal and oral administration. The highest antitrypanosomal activity was observed for inhibitors with an N-terminal 2,3-dihydrobenzo[b][1,4]dioxine group and a 4-Me-Phe residue in P2 (2e/4e) with nanomolar EC50 values (0.14/0.80 μM). The different mechanisms of reversible and irreversible inhibitors were explained using QM/MM calculations and MD simulations.

Fast-acting insulin composition comprising a substituted anionic compound and a polyanionic compound

A composition, in the form of an aqueous solution, including insulin in hexameric form, at least one substituted anionic compound of non-saccharide structure and at least one polyanionic compound other than the substituted anionic compound.

THIADIAZOLIDINEDIONES AS GSK-3 INHIBITORS

The present invention relates to new thiadiazolidinediones of formula (I), or any pharmaceutically acceptable salt, solvate or prodrug thereof, and its use in the treatment of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, particularly

THIADIAZOLIDINEDIONES AS GSK-3 INHIBITORS

The present invention relates to new thiadiazolidmediones of formula (I), or any pharmaceutically acceptable salt, solvate or prodrug thereof, and its use in the treatment of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, particularly

Process for preparing N-t-butoxycarbonylphenylalanine ester

A purified N-t-butoxycarbonylphenylalanine ester preparation having an enhanced optical activity can be obtained by bringing an N-t-butoxycarbonylphenylalanine ester preparation containing an optically active compound into contact with an aliphatic hydroc

Preparation of isocyanates from primary amines and carbon dioxide using Mitsunobu chemistry

Primary alkylamines 1 and hindered arylamines 1 give high yields of isocyanates 5 when reacted with carbon dioxide and the Mitsunobu zwitterions 4 generated from dialkyl azodicarboxylates and Bu3P in dichloromethane at - 78°C. Use of Ph3P still gave high yields of isocyanates from reactions of primary alkylamines, but only low yields were obtained from reactions of aromatic amines. Reactions which failed to give high yields of isocyanates gave either carbamoylhydrazines 6 and/or dicarbamoylhydrazines 10 and/or triazolinones 7. The triazolinones were shown to arise from reactions of reactive aryl isocyanates with the Mitsunobu zwitterion. The carbamoylhydrazines were shown not to arise from reaction of isocyanate with reduced dialkyl azodicarboxylates, and a mechanism for their formation is proposed. Single-crystal X-ray analyses confirmed the structures of 6, 7, and 10.