603121-72-8

Upstream product

• 120-20-7 2-(3,4-dimethoxyphenyl)-ethylamine 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 1064655-76-0 2-(boc)amino-N-[2-(3,4-dimethoxy-phenyl)-ethyl]-3-phenyl-propionamide 
• 1161-13-3 N-Cbz-L-Phe 
• 143439-64-9 benzyl (1S)-1-benzyl-2-{[2-(3,4-dimethoxyphenyl)ethyl]amino}-2-oxoethylcarbamate 

Downstream Products

• 54653-55-3 2-amino-N-[2-(3,4-dihydroxy-phenyl)-ethyl]-3-phenyl-propionamide 

Relevant academic research and scientific papers

C1 substituted 3, 4 - ISO-quinoline alkaloids of the preparation and its medicinal use

The invention belongs to the field of medical technology. The invention relates to a structure of the formula (I) indicated by the C1 substituted 3, 4 - ISO alkaloid or its pharmaceutically acceptable salt preparation method and medical use thereof. The invention to BOC - L - phenylalanine as raw materials, with 3, 4 - dimethoxyphenethylamine to N - acylated condensation and then remove the BOC group gets the (S)- 2 - amino - N - (3, 4 - dimethyl practiced with ethyl) - 3 - benzyl amide intermediate 1, intermediate 1 or phenethylamine derivatives with the prepared containing different substituent phenyllacetyl carries out amidation reaction, finally loop Bischler - Napieralski reaction. After activeness screening tests, the compounds of this invention possess pancrelipase inhibition, in the development into a lipase inhibitor and for preventing or treating hyperlipidemia, diabetes, obesity or metabolic syndrome and other diseases has a good application prospect.

Synthesis and in vitro studies on a potential dopamine prodrug

Dopamine delivery to the central nervous system (CNS) undergoes the permeability limitations of blood-brain barrier (BBB) which is a selective interface that excludes most water-soluble molecules from entering the brain. Neutral amino acids permeate the BBB by specific transport systems. Condensation of dopamine with neutral amino acids could afford potential prodrugs able to interact with the BBB endogenous transporters and easily enter the brain. The synthesis and characterization of the dopamine derivative 2-amino-N-[2-(3,4- dihydroxy-phenyl)-ethyl]-3-phenyl-propionamide (7) is described. The chemical and enzymatic stability of 7 was evaluated. The molecular weight (300 Da) and Log Papp (0.76) indicated that the physico-chemical characteristics of compound 7 are adequate to cross biological membranes. Compound 7 was enzymatically cleaved to free dopamine in rat brain homogenate (t1/2 = 460 min). In human plasma, the t1/2 of 7 was estimated comparable to that reported for L-DOPA. In view of a possible oral administration of 7, studies of its chemical behavior under conditions simulating those of the gastrointestinal tract showed that no dopamine production occurred; furthermore, 7 is able to permeate through a simulated intestinal mucosal membrane. The collected data suggest that compound 7 could be considered a very valuable candidate for subsequent in vivo evaluation.

Diastereoselective synthesis of 1-benzyltetrahydroisoquinoline derivatives from amino acids by 1,4 chirality transfer

L-Amino acids (L-Ala, L-Phe, L-Val, L-Pro) were used as a source of chirality in the diastereoselective synthesis of tetrahydroisoquinoline derivatives. The key step was the Pictet-Spengler condensation of ketoamides 4 and 10, which proceeded under very m