83197-70-0

Upstream product

• 6429-44-3 (S)-(-)-N-(benzyloxycarbonyl)alaninol 
• 124-63-0 methanesulfonyl chloride 
• 501-53-1 benzyl chloroformate 
• 25172-67-2 Z-Ala-O-COO-isoBu 

Downstream Products

• 1140948-93-1 (S)-2-benzyloxycarbonylaminopropyl thiolacetate 
• 1140948-95-3 Cbz-Ala-ψ[CH2SO2]-Cl 
• 1169199-21-6 Cbz-Ala-ψ[CH2SO2]-F 
• 1300858-65-4 C₁₁H₁₅NO₅S 
• 1290048-20-2 {(R)-2-[tert-Butoxycarbonyl-(3-hydroxy-propyl)-amino]-1-methyl-ethyl}-carbamic acid benzyl ester 
• 913625-37-3 (S)-6-benzyloxycarbonylamino-4-(tert-butoxycarbonyl)-4-azaheptan-1-ol 
• 1360538-90-4 (S)-6-benzyloxycarbonylamino-4-(tert-butoxycarbonyl)-4-azaheptyl methanesulfonate 
• 1360538-91-5 (S)-1-benzyl 4-tert-butyl 2-methyl-1,4-diazepane-1,4-dicarboxylate 
• 2460687-74-3 1-(4'-amino-5'-carbamoyl-1'-pyrazolyl)-(S)-2-propylbenzyloxyamide 
• 2460687-71-0 (S)-1-(4'-nitropyrazole)-2-propylbenzyloxyamide 
• 1011466-04-8 2-(S)-2-(benzyloxycarbonyl)amino-N-(tert-butoxycarbonyl)-N-(2-tert-butyldimethylsilyloxyethyl)propylamine 
• 1011466-03-7 2-(S)-2-(benzyloxycarbonyl)amino-N-(tert-butoxycarbonyl)-N-(2-hydroxyethyl)propylamine 
• 1011465-98-7 2-(S)-2-(benzyloxycarbonyl)amino-N-(tert-butoxycarbonyl)-N-(4-tert-butyldimethylsilyloxybutyl)propylamine 
• 1011465-97-6 2-(S)-2-(benzyloxycarbonyl)amino-N-(tert-butoxycarbonyl)-N-(4-hydroxybutyl)propylamine 

Relevant academic research and scientific papers

SuFExable Isocyanides for Ugi Reaction: Synthesis of Sulfonyl Fluoro Peptides

Herein, the sulfonyl fluoro isocyanides were first developed as a new type of SuFExable synthon, and they are used as building blocks in the Ugi reaction (U-4CR). The Ugi reaction was established and the substrate scope was investigated, and various sulfonyl fluoro α-amino amides and peptides could be reached in a one-step synthesis. Therefore, this protocol opens a new vision for SuFExable building blocks and click chemistry, and it also provides a distinct approach to sulfonyl fluoro peptides.

Novel sulfonamide-based carbamates as selective inhibitors of bche

A series of 14 target benzyl [2-(arylsulfamoyl)-1-substituted-ethyl]carbamates was prepared by multi-step synthesis and characterized. All the final compounds were tested for their abil-ity to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase

Chiral pyrazole derivative and synthesis method thereof

The invention belongs to the technical field of organic synthesis, and discloses a chiral pyrazole derivative and a synthesis method thereof. The chiral pyrazole derivative is (1-(4'-amino-5'-carbamoyl-1'-pyrazolyl)-(S)-2-propyl-benzyloxy amide. The synth

Synthesis and evaluation of chirally defined side chain variants of 7-chloro-4-aminoquinoline to overcome drug resistance in malaria chemotherapy

A novel 4-aminoquinoline derivative [(S)-7-chloro-N-(4-methyl-1-(4-methyl-piperazin-1-yl)pentan-2-yl)-quinolin-4-amine triphosphate] exhibiting curative activity against chloroquine-resistant malaria parasites has been identified for preclinical development as a blood schizonticidal agent. The lead molecule selected after detailed structure-activity relationship (SAR) studies has good solid-state properties and promising activity against in vitro and in vivo experimental malaria models. The in vitro absorption, distribution, metabolism, and excretion (ADME) parameters indicate a favorable drug-like profile.

IOP-lowering effect of isoquinoline-5-sulfonamide compounds in ocular normotensive monkeys

Rho-associated coiled coil-formed protein kinase (ROCK) inhibitors are under development as a new class of antiglaucoma agents. Based on the potent ROCK inhibitor H-1152, previously developed by us, we explored the possibility of related compounds as anti

NOVEL PRODUCTION METHOD FOR ISOQUINOLINE DERIVATIVES AND SALTS THEREOF

The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.

Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap

We have designed and synthesized novel irreversible serine protease inhibitors containing aliphatic sulfonyl fluorides as an electrophilic trap. These substituted taurine sulfonyl fluorides derived from taurine or protected amino acids were conveniently s

DIAZEPAM DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS

The invention is concerned with novel bicyclic compounds of Formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9 and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.

Synthesis of novel N-protected β3-amino nitriles: study of their hydrolysis involving a nitrilase-catalyzed step

Several commercially available nitrilases were investigated with regard to their potential to hydrolyze N-protected β3-amino nitriles into their corresponding N-protected β3-amino acids. The biotransformations were obtained in different proportions depending on the nitrilase involved. The best hydrolysis results were achieved for the N-Cbz-β3-amino nitrile from l-alanine using the NIT-107, in a phosphate buffer at 0.05 M. However, no biotransformation into the corresponding acids was observed for the N-sulfonylamide β3-amino nitriles. Two simple and efficient procedures to prepare the β3-amino nitriles from their analogous α-amino acids are described. Thirty four new substances were synthesized and characterized over the course of this work.

Synthesis of β-aminoethanesulfonyl fluorides or 2-substituted taurine sulfonyl fluorides as potential protease inhibitors

Substituted taurine sulfonyl fluorides derived from taurine or protected amino acids are conveniently synthesized from β-aminoethanesulfonyl chlorides using KF/18-crown-6 or from β-aminoethanesulfonates using DAST.