72500-24-4

Upstream product

• 501-53-1 benzyl chloroformate 
• 147-85-3 L-proline 
• 1148-11-4 N-Benzyloxycarbonyl-L-proline 
• 6216-63-3 N-Cbz-Prolinol 
• 98-59-9 p-toluenesulfonyl chloride 
• 23356-96-9 (S)-1-Pyrrolidin-2-yl-methanol 

Downstream Products

• 956108-36-4 (S)-2-(quinolin-6-yloxymethyl)-pyrrolidine-1-carboxylic acid benzyl ester 
• 385802-14-2 (2S)-2-[(2-methoxybenzylamino)methyl]pyrrolidine-1-carboxylic acid benzyl ester 
• 1140458-77-0 benzyl (S)-2-{[1-(ethoxycarbonyl)-1-methylethoxy]methyl}pyrrolidine-1-carboxylate 
• 119020-03-0 2-(S)-aminomethyl-pyrrolidine-1-carboxylic acid benzyl ester 
• 133963-43-6 [3R-(1(S^*),3α,4α)]-3-(acetyloxy)-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-1-(2-pyrrolidinylmethyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 128510-26-9 <3R-<1(S^*),3α,4α>>-3-(acetyloxy)-1-<<(benzyloxycarbonyl)-2-pyrrolidinyl>methyl>-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 851394-30-4 5-[(S)-1-pyrrolidin-2-ylmethyl]-1H-tetrazole 
• 851394-29-1 2-(1H-tetrazol-5-ylmethyl)-pyrrolidine-1-carboxylic acid benzyl ester 
• 141774-67-6 (S)-benzyl 2-(azidomethyl)pyrrolidine-1-carboxylate 
• 134932-93-7 <3R-<1(S^*),3α,4α>>-1-<<(benzyloxycarbonyl)-2-pyrrolidinyl>methyl>-1,3,4,5-tetrahydro-3-hydroxy-4-(4-methoxyphenyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 72500-25-5 (S)-benzyl 2-(cyanomethyl)pyrrolidine-1-carboxylate 
• 128573-92-2 [3R-(1(S^*),3α,4α)]-3-hydroxy-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-1-(2-pyrrolidinylmethyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 1321848-92-3 benzyl (S)-2-((3-(3,5-bis(trifluoromethyl)phenyl)thioureido)methyl)pyrrolidine-1-carboxylate 
• 1227910-54-4 phenylmethyl (2R)-2-ethyl-1-pyrrolidinecarboxylate 

Relevant academic research and scientific papers

The highly enantioselective bifunctional organocatalysts for the Michael addition of сyclohexanone to titroolefins

A new family of organocatalyst derived from proline has been developed and shown to be an efficient catalyst for asymmetric Michael addition of cyclohexanone to nitroolefins with high diastereo- and enanthio -selectivities. (syn: anti ratio up to 99:1, ee

Highly Enantioselective Reactions of Cyclohexanone and β,γ-Unsaturated α-Keto Ester: The Tuning of Chemo-selectivities by Secondary and Primary Amine Catalysts

A series of of amphiphilic imidazole based secondary and primary amine catalysts were synthesized and shown to be very effective with an acid cocatalyst for the asymmetric reaction of cyclohexanone to β,γ-unsaturated α-keto ester. Interestingly, primary a

(S)-2,2,6,6-Tetramethyl-N-(pyrrolidin-2-ylmethyl)piperidin-4-amine as an efficient organocatalyst for asymmetric Michael addition

new organocatalyst derived from proline has been developed and shown to be an efficient catalyst for asymmetric Michael addition reactions of cyclohexanone to nitroolefins with high diastereo- and enantio -selectivities.

Synthesis of chiral NADH analog based on proline template including thiourea and nicotinic acid moieties

Chiral reductase-mimicking organic molecule built on proline template incorporating a covalently bound NADH mimic via thiourea, and related reducing agent Hantzsch dihydropyridine, was designed. A synthetic path was developed involving interlinking of chiral proline derivatives with thiourea and subsequent coupling reaction with nicotinoyl chloride. The structure of target compound was studied by x-ray, indicating a double H bond with thiourea hydrogens and oxygen O1 of benzylcarbamate fragment. The reduction of benzil and imines was performed. Taylor & Francis Group, LLC.

CHEMICAL COMPOUNDS

The invention is directed to 6-(4-pyι?midinyl)-1 H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1 - R4 are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

CHEMICAL COMPOUNDS

The invention is directed to to substituted indazole derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 - R6 and X are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically leukemia and cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Asymmetric organocatalysis of the addition of acetone to 2-nitrostyrene using N-diphenylphosphinyl-1,2-diphenylethane-1,2-diamine (PODPEN)

The highly enantioselective addition of acetone to 2-nitrostyrene, using N-diphenylphosphinyl-trans-1,2-diphenylethane-1,2-diamine (PODPEN) as a catalyst, is described.

Aspects of the synthesis of an exceptionally preorganized self-immolative spacer-phenolate unit

This study introduces a highly preorganized self-immolative spacer that is coupled to a nonfluorescent leaving group. The water-soluble compound can rapidly liberate a water-insoluble fluorescent precipitate by intramolecular attack of a free amine on a phenolic ester group via a six-membered transition state. One of the crucial steps in the synthesis of this molecule was a sterically very unfavored nucleophilic substitution to create a tertiary ether; this was optimized using model compounds. Another key challenge was deprotection by catalytic hydrogenation at low temperatures in order to furnish the hydroacetate of the free amine without further fragmentation. LC-MS and fluorescence studies showed that this compound collapsed instantaneously in methanol, as well as within a wide pH range in buffered aqueous media. Georg Thieme Verlag Stuttgart · New York.

Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands

A series of nicotinic ligands, carrying a quinoline nucleus, and characterized by a pharmacophoric distance between the quinoline nitrogen (H-bond acceptor) and the cationic nitrogen atoms higher than that proposed in the classical pharmacophoric models,

A homo-proline tetrazole as an improved organocatalyst for the asymmetric Michael addition of carbonyl compounds to nitro-olefins

A new homo-proline tetrazole derivative 7 has been prepared and shown to have improved properties for achieving asymmetric Michael addition of carbonyl compounds to nitro-olefins.