145730-69-4

Upstream product

• 16217-15-5 1-benzyloxycarbonyl-4-oxo-L-proline methyl ester 
• 200184-60-7 (S)-N-benzyloxycarbonyl-4-methylenepyrrolidine-2-carboxylic acid methyl ester 
• 7517-19-3 methyl (L)-leucinate hydrochloride 
• 1353864-33-1 C₂₀H₃₂N₂O₄Si 
• 1353864-31-9 C₂₀H₃₄N₂O₄Si 
• 55094-98-9 D‐α‐hydroxyglutaric acid 
• 6893-26-1 D-Glutamic acid 

Downstream Products

• 1353864-37-5 N-Boc-trans-4-methyl-L-proline benzyl ester 
• 138512-74-0 1-tert-butyl 2-methyl (2S,4R)-4-methylpyrrolidine-1,2-dicarboxylate 

Relevant academic research and scientific papers

Highly stereoselective gram scale synthesis of all the four diastereoisomers of Boc-protected 4-methylproline carboxylates

A general and practical synthetic process for all the four diastereoisomers of Boc-protected 4-methylproline carboxylates has been developed with essentially complete stereoselectivity on the gram scale, which represents the most diastereoselective preparation of 4-methylproline derivatives to date. This synthesis features an Evans asymmetric alkylation to elegantly establish the challenging stereochemistry of the 4-methyl group, providing valuable insights for the diastereoselective preparation of 4-substituted prolines.

Highly efficient syntheses of azetidines, pyrrolidines, and indolines via palladium catalyzed intramolecular amination of C(sp3)-H and C(sp2)-H bonds at γ and δ positions

Efficient methods have been developed to synthesize azetidine, pyrrolidine, and indoline compounds via palladium-catalyzed intramolecular amination of C-H bonds at the γ and δ positions of picolinamide (PA) protected amine substrates. These methods feature relatively a low catalyst loading, use of inexpensive reagents, and convenient operating conditions. Their selectivities are predictable. These methods highlight the use of unactivated C-H bond, especially the C(sp3)-H bond of methyl groups, as functional groups in organic synthesis.

BICYCLIC UNSATURATED TERTIARY AMINE COMPOUND

The present invention provides a bicyclic unsaturated tertiary amine compound capable of inhibiting the production of inflammatory cytokines.A compound of the following formula (1): (wherein, A represents pyrrole or pyrazole, R1 represents an aryl group or a heteroaryl group which may be substituted, R2 represents a heteroaryl group which may be substituted, and R3 represents an indolizine group), or a pharmacologically acceptable salt thereof, a pharmacologically acceptable ester thereof or other pharmacologically acceptable derivative thereof.

Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses

Compounds having activity against production of an inflammatory cytokine of formula (I)′: 1A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is (IIa)′, (IIb)′ or (IIc)′: 2m′ is 1; E′ is nitrogen; D′ is >C(R5′)—, R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 5-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′ is hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′ is alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′ is oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.

COMPOUNDS SUBSTITUTED WITH BICYCLIC AMINO GROUPS

[Object]The object of the present invention is to provide compounds which are able to inhibit the production of inflammatory cytokines.[Solution]Compounds of the general formula (I) below, or pharmacologically acceptable salts, esters or other derivatives