169604-92-6

Upstream product

• 77087-60-6 methyl (S)-2-amino-3-tert-butoxycarbonylaminopropanoate 
• 98-59-9 p-toluenesulfonyl chloride 
• 16947-86-7 N^α-Tosyl-N^β-(tert-butpxycarbonyl)-L-α,β-diamonopropionic acid 
• 74-88-4 methyl iodide 
• 21753-19-5 2-(S)-p-toluenesulfonylamino-β-alanine 
• 36212-66-5 N²-(toluene-4-sulfonyl)-L-asparagine 
• 58457-98-0 methyl (2S)-2-{[(benzyloxy)carbonyl]amino}-3-[(tert-butoxycarbonyl)amino]propanoate 

Downstream Products

• 113299-00-6 L-2-p-Toluolsulfonylamino-3-amino-propionsaeure-methylester 
• 80312-88-5 tert-butyl 2S-(3-hydroxy-2-((4-methylphenyl)sulfonamido)propyl)carbamate 
• 80312-73-8 (S)-3-amino-2-(4-toluenesulfonyl)amino-1-propanol 
• 199853-74-2 4-Methyl-N-[(R)-1-methyl-4-(3-methyl-benzyl)-[1,4]diazepan-6-yl]-benzenesulfonamide 
• 199853-73-1 4-Methyl-N-[(R)-4-methyl-1-(3-methyl-benzyl)-2-oxo-[1,4]diazepan-6-yl]-benzenesulfonamide 
• 199853-72-0 (S)-N-methyl-N-[3-(3-methylbenzyl)-amino-2-(4-toluenesulfonyl)amino-1-propyl]aminoacetic acid 
• 199853-76-4 N-[(S)-3-Hydroxy-2-(toluene-4-sulfonylamino)-propyl]-2-methylamino-N-(3-methyl-benzyl)-acetamide 
• 199853-70-8 (S)-3-[N-(3-methylbenzyl)-N-trifluoroacetylaminomethyl]-1-(4-toluenesulfonyl)aziridine 
• 199853-69-5 (S)-3-[N-(3-methylbenzyl)-N-trifluoroacetyl]amino-2-(4-toluenesulfonyl)amino-1-propanol 
• 199853-67-3 {[[(S)-3-Hydroxy-2-(toluene-4-sulfonylamino)-propyl]-(3-methyl-benzyl)-carbamoyl]-methyl}-methyl-carbamic acid tert-butyl ester 
• 199853-71-9 ethyl (S)-N-methyl-N-{3-[N-(3-methylbenzyl)-N-trifluoroacetyl]amino-2-(4-toluenesulfonyl)amino-1-propyl}aminoacetate 
• 199853-65-1 (S)-3-(3-methylbenzyl)amino-2-(4-toluenesulfonyl)amino-1-propanol 
• 169604-94-8 (S)-3-(3-Chloromethyl-benzoylamino)-2-(toluene-4-sulfonylamino)-propionic acid methyl ester 
• 169604-95-9 (S)-3-[3-(4-Cyano-phenoxymethyl)-benzoylamino]-2-(toluene-4-sulfonylamino)-propionic acid methyl ester 

Relevant academic research and scientific papers

Design, synthesis, and in vitro activities of benzamide-core glycoprotein IIb/IIIa antagonists: 2,3-Diaminopropionic acid derivatives as surrogates of aspartic acid

In an effort to discover novel nonpeptide glycoprotein IIb/IIIa (GPIIb/IIa, α(IIb)/β3) inhibitors, we investigated RGD mimetics featuring a 3-substituted benzoic acid as the core, benzamidine as the basic moiety, and a series of β- and α-substituted β-alanine derivatives as aspartic acid surrogates. It was found that the use of β-methyl β-alanine slightly improved the anti-aggregant potency in human platelet-rich plasma over the unsubstituted β-alanine compound, while β-substitution with a trifluoromethyl group resulted in considerable loss in activity. Significant enhancement (up to 100-fold) in potency was obtained when the β-alanine was replaced with N2-substituted L-2,3-diaminopropionic acid derivatives. Among the three types of α-substituents (carbamate, amide, and sulfonamide) investigated, no apparent preference was observed with respect to in vitro potency. However, alkyl groups were more favorable than arylalkyl groups (Cbz) in the carbamate analogues. We also investigated piperidine, piperazine, and N-formamidinopiperidine as replacements for the benzamidine moiety. The former two replacements led to a drop in potency while the latter replacement resulted in maintenance of activity as compared with the corresponding benzamidine analogue.

Asymmetric synthesis of (R)-6-amino-1-methyl-4-(3-methyl- benzyl)hexahydro-1H-1,4-diazepine from L-asparagine

An efficient asymmetric synthesis of (R)-6-amino-1-methyl-4-(3- methylbenzyl)hexahydro-1H-1,4-diazepine [(R)-2] which serves as the amine part of (R)-1, a potent and selective 5-HT3 receptor antagonist, is described. Formation of the hexahydro-

Design, synthesis and in vitro activities of a series benzimidazole/benzoxazole glycoprotein IIb/IIIa inhibitors

A potent centrally constrained series of benzimidazole and benzoxazole glycoprotein IIb/IIIa inhibitors has been discovered based on the solution conformation of a cyclic RGD-containing peptide, DMP 728. The high potency of this series of compounds in the inhibition of platelet aggregation requires a benzamidine as the basic moiety and an α-carbamate or sulfonamide substituted β-alanine as the acidic moiety.