29802-26-4

Upstream product

• 66605-57-0 (S)-N-tert-butoxycarbonyl-2-amino-3-phenylpropanol 
• 78800-68-7 (S)-tert-butyl 1-(dimethylamino)-1-oxo-3-phenylpropan-2-ylcarbamate 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 123665-42-9 (S)-2-Amino-N,N-dimethyl-3-phenyl-propionamide hydrochloride 
• 126301-19-7 (2S)-2-[(tert-butoxycarbonyl)amino]-3-phenylpropyl methanesulfonate 
• 51987-73-6 (S)-2-tert-butoxycarbonylamino-3-phenyl-propionic acid methyl ester 
• 3182-95-4 L-Phenylalaninol 
• 141403-49-8 (2S)-2-[N-(tert-butoxycarbonyl)amino]-3-phenyl-O-(4-methylphenylsulfonyl)propan-1-ol 
• 29618-17-5 L-phenylalanine dimethylamide 
• 340161-69-5 tert-butyl (S)-(1-(dimethylamino)-3-phenylpropan-2-yl)carbamate 

Downstream Products

• 259537-56-9 Benzyl 2-[3-[(3-[(tert-butoxycarbonyl)(methyl)amino]methylphenethyl)amino]-5-chloro-6-methyl-2-oxo-1(2 H)-pyrazinyl]acetate 
• 943238-77-5 C₂₆H₂₇N₃O₅ 
• 943238-87-7 C₂₈H₃₅N₃O₃ 
• 1048692-53-0 (S)-1-(3,5-bis(trifluoromethyl)phenyl)-3-(1-(dimethylamino)-3-phenylpropan-2-yl)thiourea 
• 1438263-84-3 (S)-N-(4-bromobenzyl)-N,N-dimethyl-2-(3-(4-nitrophenyl)thioureido)-3-phenylpropan-1-ammonium bromide 
• 340161-69-5 tert-butyl (S)-(1-(dimethylamino)-3-phenylpropan-2-yl)carbamate 
• 943238-88-8 C₂₈H₃₃N₃O₃ 
• 1308662-08-9 2-{3-[((S)-1-dimethylaminomethyl-2-phenyl-ethylamino)-methyl]-benzyl}-1,1-dioxo-1λ6-isothiazolidine-3-carboxylic acid ethyl ester 
• 1308661-88-2 2-(3-{[(2,3-difluoro-6-methoxy-benzyl)-((S)-1-dimethylaminomethyl-2-phenyl-ethyl)-amino]-methyl}-benzyl)-1,1-dioxo-1λ6-isothiazolidine-3-carboxylic acid((1S,2S,3S,5R)-2,6,6-trimethyl-bicyclo[3.1.1]hept-3-yl)-amide 
• 1308661-80-4 2-(3-{[(6-chloro-2-fluoro-3-methoxy-benzyl)-((S)-1-dimethylaminomethyl-2-phenyl-ethyl)-amino]-methyl}-benzyl)-1,1-dioxo-1λ6-isothiazolidine-3-carboxylic acid ((1S,2S,3S,5R)-2,6,6-trimethyl-bicyclo[3.1.1]hept-3-yl)-amide 
• 1308662-10-3 2-{3-[((S)-1-dimethylaminomethyl-2-phenyl-ethylamino)-methyl]-benzyl}-1,1-dioxo-1λ6-isothiazolidine-3-carboxylic acid ((1S,2S,3S,5R)-2,6,6-trimethyl-bicyclo[3.1.1]hept-3-yl)amide 
• 1308662-09-0 2-{3-[((S)-1-dimethylaminomethyl-2-phenyl-ethylamino)-methyl]-benzyl}-1,1-dioxo-1λ6-isothiazolidine-3-carboxylic acid 
• 300547-19-7 1-[(1S)-1-Benzyl-2-(dimethylamino) ethyl]-3-(2-hydroxyethyl)-3-phenethyl urea 
• 1009091-91-1 C₄₈H₆₇N₅O₆ 

Relevant academic research and scientific papers

PD(II)-CATALYZED ENANTIOSELECTIVE C-H ARYLATION OF FREE CARBOXYLIC ACIDS

The invention includes procedures for stereoselective β-arylation of carboxylic acids having a β-carbon atom. For example, stereoselective arylation procedures include the following reactions: (I)

Pd(II)-Catalyzed Enantioselective C(sp3)-H Arylation of Free Carboxylic Acids

A monoprotected aminoethyl amine chiral ligand based on an ethylenediamine backbone was developed to achieve Pd-catalyzed enantioselective C(sp3)-H arylation of cyclopropanecarboxylic and 2-aminoisobutyric acids without using exogenous directing groups. This new chiral catalyst affords new disconnection for preparing diverse chiral carboxylic acids from simple starting materials that are complementary to the various ring forming approaches.

Asymmetric hydroazidation of α-substituted vinyl ketones catalyzed by chiral primary amine

We report herein the first example of asymmetric hydroazidation of α-substituted vinyl ketones by using chiral primary amines as the catalysts. A simple chiral primary-tertiary diamine catalyst derived from L-phenylalanine was found to readily promote this aza-Michael addition reaction with enamine protonation as the key stereogenic step, thus enabling the effective synthesis of α-chiral β-azido ketones with good yields and moderate enantioselectivities.

Synthesis and antimalarial activity of new 4-aminoquinolines active against drug resistant strains

In the present study we have synthesized a new class of 4-aminoquinoline derivatives via replacement of the diethylamine functionality of chloroquine (CQ) with acyclic and/or cyclic amine groups containing basic tertiary terminal nitrogen and bioevaluated them for antimalarial activity against Plasmodium falciparum in vitro (CQ-sensitive strain-3D7 & CQ-resistant strain-K1) and Plasmodium yoelii in vivo (N-67 strain). Among the series, thirteen compounds showed superior antimalarial activity against K1 strain as compared to CQ. In addition, all these analogs showed 100% suppression of parasitaemia on day 4 in the in vivo mouse model against N-67 strain when administered orally. Further, biophysical studies suggest that these compounds act on the heme polymerization target.

Novel bifunctional thiourea-ammonium salt catalysts derived from amino acids: Application to highly enantio- and diastereoselective aza-Henry reaction

The development of new efficient and easily accessible catalysts has been one of the focuses in asymmetric phase-transfer catalysis. In this paper, a novel class of chiral bifunctional thiourea-ammonium phase-transfer catalysts were synthesized from commercially available α-amino acids. The structural modularity of these catalysts permits facile tunings to achieve optimum results, which was demonstrated in catalyzing the aza-Henry reaction with excellent enantioselectivities (up to 99.5% ee) and diastereoselectivities (up to >25:1 dr).

BICYCLIC AZAHETEROCYCLIC CARBOXAMIDES AS INHIBITORS OF THE KINASE P70S6K

The invention provides novel bicyclic azaheterocyciic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

SULTAM DERIVATIVES

The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.

Ring-Opening polymerization of lactides catalyzed by natural Amino-Acid based zinc catalysts

A series of chiral NNO-tridentate Schiff base ligands derived from natural amino acids were reacted with zinc(bis-trimethylsilylamide)2 to provide metal complexes which have been fully characterized. One of these derivatives was further reacted

Novel bifunctional chiral urea and thiourea derivatives as organocatalysts: Enantioselective nitro-Michael reaction of malonates and diketones

A modular synthesis of novel bifunctional urea and thiourea organocatalysts derived from cheap, easily accessible natural and non-natural amino acids was reported. The generality of the synthesis was demonstrated in the preparation of catalysts 4a-i in th

Organocatalyzed highly enantioselective michael additions of malonates to enones by using novel primary-secondary diamine catalysts

A novel primary-secondary diamine catalyst readily available from primary amino acids in three steps for the highly enantioselective Michael additions of malonates to α,β-unsaturated ketones was reported. The Michael reaction of dimethyl malonate with benzylideneacetone was selected as a model reaction for catalyst evaluation. The length of the alkyl chain is found to influence the catalytic abilities of the catalysts and the n-propylated catalyst gave the highest yield and ee value. The addition of a series of malonates to enone performed under the optimized conditions is found to be sensitive to the steric hinderance on the malonates. Heterocyclic furan enone is found to perform well to give the desired product in 92% yield and 99% ee, while no decrease in yield and ee value is observed for sterically hindered enone.