96145-91-4

Upstream product

• 151-56-4 ethyleneimine 
• 5817-26-5 ethyl (2S)-pyrrolidine-2-carboxylate 
• 917886-64-7 (S)-1-(2-Amino-ethyl)-pyrrolidine-2-carboxylic acid 
• 675824-95-0 (S)-methyl 1-(2-((tert-butoxycarbonyl)amino)ethyl)pyrrolidine-2-carboxylate 
• 147-85-3 L-proline 
• 350028-10-3 (2S,11S,20S)-2,6-cyclo-11,15-cyclo-20,24-cyclo-26-(benzyloxycarbonylamino)-6,9,15,18,24-pentaaza-10,19-dioxohexacosanoic acid methyl ester 
• 350028-08-9 (S)-1-(2-{[(S)-1-(2-Amino-ethyl)-pyrrolidine-2-carbonyl]-amino}-ethyl)-pyrrolidine-2-carboxylic acid methyl ester 
• 83283-35-6 Proline tert-butyl ester dibenzenesulfimide salt 
• 917886-62-5 (S)-1-(2-tert-butoxycarbonylaminoethyl)pyrrolidine-2-carboxylic acid tert-butyl ester 

Downstream Products

• 93643-24-4 (S)-octahydropyrrolo[1,2-a]pyrazine 
• 49864-70-2 L-10-<β-N-(1,4-Diazabicyclo<4.3.o>nonanyl)propionyl>-2-chlorophenothiazine 

Relevant academic research and scientific papers

PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS

There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein: X represents a nitrogen atom; Y represents -C(H2)-, (-C(H2)-)2, -S(O2)- or -C(=O)-; Z represents -C(H2)-, -S(O2)-, -N(Rz)-, or an oxygen or sulphur atom; A represents hydrogen or -CH2OH; Rz represents hydrogen, C1-6 alkyl, C1-6 alkoxy, -COR7 or -SO2R7; R1 represents halogen, C1-6 alkyl, C1-6 alkoxy, =O, haloC1-6 alkyl, haloC1-6 alkoxy, hydroxyl or -CH2OH; m represents an integer from 0 to 3; R2 represents halogen, =O, C1-6alkyl (optionally substituted by one or more hydroxyl groups), -COOR7, -CONR7R8, C1-6 alkoxy, haloC1-6 alkyl, haloC1-6alkoxy or C1-6 alkyloC1-6 alkyl; n represents an integer from 0 to 3; p and q independently represent an integer from 0 to 2; R3 represents an -aryl, -heteroaryl, -heterocyclyl, -aryl-aryl, -aryl-heteroaryl, -aryl-heterocyclyl, -heteroaryl-aryl, -heteroaryl-heteroaryl, -heteroaryl-heterocyclyl, -heterocyclyl-aryl, -heterocyclyl-heteroaryl or -heterocyclyl-heterocyclyl group, all of which may be optionally substituted by one or more (e.g. 1, 2 or 3) halogen, C1-6 alkyl (optionally substituted by one or more hydroxyl groups), C3-8cycloalkyl, C1-6 alkoxy, hydroxyl, haloC1-6alkyl, haloC1-6 alkoxy, cyano, -S-C1-6 alkyl, -SO-C1-6 alkyl, -SO2-C1-6 alkyl, -COR7, -CONR7R8, -NR7R8, -NR7COC1-6 alkyl, -NR7SO2-C1-6alkyl, C1-6 alkyl-NR7R8, -OCONR7R8 , -NR7CO2R8 or -SO2NR7R8 groups; R4 and R5 independently represent C1-6 alkyl, or R4 and R5 together with the carbon atom to which they are attached may together form a C3-8cycloalkyl group; R6 represents halogen, C1-6 alkyl, C3-8cycloalkyl, C1-6 alkoxy, haloC1-6 alkyl or haloC1-6 alkoxy; s represents an integer from 0 to 4; R7 and R8 independently represent hydrogen, C1-6 alkyl or C3-8cycloalkyl; or solvates thereof.

Synthesis of δ-lactam (2-oxopiperazine) inhibitors of elastase

Different routes for the synthesis of N-sulfonyl derivatives of δ-lactam (2-oxopiperazine) inhibitors of the serine protease elastase were evaluated.

The synthesis of L-proline derived hexaazamacrocyclic ligands of C3 symmetry via intramolecular methyl ester aminolysis

A convenient synthesis of enantiomerically pure 18-, 21-, and 24-membered hexaaza-crown ligands is presented. Linear α,ω-aminoesters, prepared from L-proline, undergo intramolecular aminolysis to afford the corresponding 18-, 21-, and 24-membered macrocyc