294888-41-8

Upstream product

• 6747-15-5 α-amino-(+/)-3-indoleacetic acid 
• 501-53-1 benzyl chloroformate 
• 110317-48-1 methyl 2-amino-2-(1H-indol-3-yl)acetate 
• 113975-75-0 methyl indol-3-ylglyoxylate oxime 
• 18372-22-0 2-(3-indolyl)oxoacetic acid methyl ester 

Downstream Products

• 294888-42-9 N-Cbz-indol-3-yl-N-methyl-O-methoxyglycinamide 
• 294888-39-4 (+/-)-methyl-N-benzyloxycarbonyl-3-indoleglycinate 
• 470670-73-6 2,5-dioxo-4-[1-(toluene-4-sulfonyl)-1H-indol-3-yl]-oxazolidine-3-carboxylic acid benzyl ester 
• 470670-87-2 (+/-)-N-benzyloxycarbonyl-1-tosyl-3-indoleglycine 
• 470670-88-3 (+/-)-methyl-N-benzyloxycarbonyl-1-tosyl-3-indoleglycinate 

Relevant academic research and scientific papers

Novel synthesis method of indole glycinate

The invention relates to a novel synthesis method of indole glycinate. A substituted indole glycinate derivative 3 is obtained after indole 1, acylamino malonate 2 and an oxidant as raw materials are heated to 60-100 DEG C in an organic solvent under the protection of nitrogen and are subjected to a cross dehydrogenation coupling reaction, an obtained product is treated and subjected to hydrolysis and decarboxylation under the alkaline condition, a product 4 is obtained and subjected to hydrolysis deprotection under the alkaline condition, and a final indole glycinate product 5 is obtained through acidification. Indole 1, acylamino malonate 2 and the oxidant are taken as the raw materials, the raw materials are cheap and easy to obtain, a substrate range is wide, the compatibility of a functional group is good, and final indole glycinate can be obtained in a higher yield from various substituted indole and acylamino malonate. The method has multiple advantages that the synthesis route is short, the reaction raw materials are low in toxicity, separation and purification are convenient and the like, and has great practical application value in synthesis of the compounds.

Development of a rapid, room-temperature dynamic kinetic resolution for efficient asymmetric synthesis of α-aryl amino acids

equation presented A rapid, highly efficient and general dynamic kinetic resolution (DKR) of racemic α-aryl UNCAs with the dual-function catalysis of modified cinchona alkaloid was accomplished at room temperature. This DKR led to the development of a highly enantioselective catalytic method for the practical synthesis of a wide range of α-aryl and α-heteroaryl amino acids in 89-92% ee and 86-95% yield from racemic UNCAs.

Syntheses of bis(3'-indolyl)-2(1H)-pyrazinones

The syntheses of 3,6-bis(3'-indolyl)-2(1H)-pyrazinone and 3,5- bis(3'indolyl)-2(1H)-pyrazinone were described. Syntheses of 3,6-bis(3'- indolyl)-2(1H)-pyrazinone proceeded through the condensation of N-Boc- indolylglycine with indol-3-yl-N-methyl-O-methox