14891-08-8

Upstream product

• 3783-61-7 diethyl 2-azabutane-1,4-dicarboxylate 
• 541-41-3 chloroformic acid ethyl ester 
• 140-88-5 ethyl acrylate 
• 4143-07-1 ethyl 3-<(ethoxycarbonyl)amino>propionate 

Downstream Products

• 1438-38-6 ethyl 1-ethoxycarbonyl-3-oxo-pyrrolidine-2-carboxylate 
• 3751-82-4 ethyl 1-ethoxycarbonyl-4-oxopyrrolidine-3-carboxylate 
• 83455-93-0 (+/-)-3β-(benzyloxy)-1-(ethoxycarbonyl)-2β-(prop-1-en-3-yl)pyrrolidine 

Relevant academic research and scientific papers

Method for preparing 3-(3-chloropropyl)-4-oxopyrrolidine-1-ethyl carboxylate

The invention provides a novel method for preparing 3-(3-chloropropyl)-4-oxopyrrolidine-1-ethyl carboxylate, aiming at solving the technical problems of a traditional 3-(3-chloropropyl)-4-oxopyrrolidine-1-ethyl carboxylate synthesis method in the prior art that a flow is complicated, the environmental hazards are great, the safety is low and the yield is low. The technology takes glycine ethyl ester and ethyl acrylate as starting raw materials, and steps of taking benzylamine as a raw material and carrying out debenzylation in a subsequent process are reduced; a process for preparing the 3-(3-chloropropyl)-4-oxopyrrolidine-1-ethyl carboxylate is greatly simplified; an existing technology needs 6-step reaction, and the technology only needs 5-step reaction, so that the operation is simplified and a production period is shortened; the method is applicable to large-scale industrial production. The technology does not take the benzylamine as the starting raw material, and the generation ofa cancer-causing high-hazard substance, i.e., benzyl chloride, is directly stopped from the source; harms to an ecological environment and body health of people are effectively avoided; a reaction process is safe and accords with environmental protection requirements of China better; the total yield is greatly improved and the yield is greater than or equal to 50 percent.

2-AMINO PYRIMIDINE COMPOUNDS AS POTENT HSP-90 INHIBITORS

The present invention is directed to compounds of formula (I), or pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.

2-AMIN0-5, 7-DIHYDR0-6H- PYRROLO [3, 4-D] PYRIMIDINE DERIVATIVES AS HSP-90 INHIBITORS FOR TREATING CANCER

The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.

Certain 2-carboxypiperidyl-alkylene phosphonic acids and esters thereof useful for the treatment of disorders responsive to N-methyl-D-aspartate receptor blockade

The present invention is concerned with the phosphonic acids of formula I STR1 wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

A NOVEL AND STEREOSELECTIVE SYNTHESIS OF CIS-1-8-H-HYDROXYPYRROLIZIDINE

The title compound was synthesized through a regioselective introduction of allyl group at the C2 position of the 3-oxopyrrolidine derivative (2) by sigmatropic rearrangement and an amino cyclization via the episulfonium intermediate (8)