145232-15-1

Upstream product

• 14173-40-1 2-amino-3-(4-chlorophenyl)propionic acid methyl ester hydrochloride 
• 7424-00-2 DL-Phe(4Cl) 
• 119744-86-4 tert-butyl (S)-[1-amino-3-(4-chlorophenyl)-1-oxopropan-2-yl]carbamate 
• 14173-40-1 (S)-2-amino-3-(4-chloro-phenyl)-propionic acid methyl ester hydrochloride 
• 51301-86-1 Boc-p-chloro-L-Phe-OH 

Downstream Products

• 928342-09-0 Boc-Trp-(p-Cl-Phe)-NH₂ 
• 928342-10-3 Boc-Gly-Trp-(p-Cl-Phe)-NH₂ 
• 928342-13-6 N^α-(N,N'-bis-benzyloxycarbonyl)amidino-Tyr(Me)-D-Pro-Gly-Trp-(p-Cl-Phe)-NH2 
• 1014607-97-6 C₅₂H₅₃ClN₈O₉ 
• 145232-14-0 3-tert-butoxycarbonylamino-N-[1-carbamoyl-2-(4-chloro-phenyl)-ethyl]-succinamic acid benzyl ester 
• 104907-20-2 1,2-diamino(4-chlorobenzyl)ethane 

Relevant academic research and scientific papers

Control of 6-Exo and 7-Endo cyclizations of alkynylamides using platinum and bismuth catalysts

The rules of cyclization: Alkynylamides are regioselectively cycloisomerized into piperazin-2-one and 1,4-diazepan-2-one derivatives by using catalytic amounts of appropriate metal catalysts. A 6-exo-dig addition proceeds in the presence of Bi(OTf)3, while the 7-endo-dig addition occurs with PtCl2 for the same substrate. (see scheme; Ns=o- nitrobenzenesulfonyl, Ts=p-toluenesulfonyl, Cbz=benzyloxycarbonyl, DCE=dichloroethane) Copyright

Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: Design, synthesis, and pharmacological characterization

We synthesized four new analogs of endomorphin-1 by systematic chemical modifications. To identify the best possible drug candidates for clinical pain management and to investigate the potential contribution of these alterations to the biological activity, their pharmacological properties were determined. All of the analogs showed significantly enhanced metabolic stability. The fact that centrally mediated analgesia following peripheral administration was observed with one of the analogs suggested the approach design undertaken here had validity in the development of endomorphin-1 as a successful opioid drug for the clinic.