141222-95-9

Upstream product

• 121492-10-2 N-phenyl-N-(tert-butoxtcarbonyl)-2-aminoethanol 
• 24424-99-5 di-tert-butyl dicarbonate 
• 122-98-5 2-Anilinoethanol 
• 169268-95-5 tert-butyl allyl(phenyl)carbamate 

Downstream Products

• 955124-13-7 C₁₇H₂₃NO₄ 
• 148701-50-2 N-Boc-2-hydroxy-1-phenyl-hex-5-enyl-1-amine 
• 1218764-59-0 tert-butyl (3R,4R)-4-({2-[(tert-butoxycarbonyl)(phenyl)amino]ethyl}amino)-3-(3,4-dichlorophenyl)piperidine-1-carboxylate 
• 1218764-61-4 tert-butyl (3R,4R)-3-(3,4-dichlorophenyl)-4-{[2-(phenylamino)ethyl]amino}piperidine-1-carboxylate 
• 1218760-04-3 tert-butyl (3R,4R)-3-(3,4-dichlorophenyl)-4-(2-oxo-3-phenylimidazolidin-1-yl)piperidine-1-carboxylate 
• 85692-23-5 4-anilinocrotonic acid ethyl ester 

Relevant academic research and scientific papers

Silver-Catalyzed Three-Component 1,1-Aminoacylation of Homopropargylamines: α-Additions for Both Terminal Alkynes and Isocyanides

The reaction of secondary homopropargylamines, isocyanides, and water in the presence of a catalytic amount of silver acetate and subsequent purification by chromatography on silica gel afforded substituted proline amides in good to excellent yields. Primary homopropargylamines underwent a cyclizative Ugi–Joullié three-component reaction with isocyanides and carboxylic acids to afford functionalized N-acyl proline amides. High diastereoselectivity was observed in the synthesis of 4-alkoxy and 4,5-disubstituted proline derivatives. This work represents the first examples of a three-component cyclizative 1,1-aminoacylation of terminal alkynes.

Use of the composite material RuO2/BaTi4O9 as an environmentally benign solid catalyst for the oxidative cleavage of olefins

Catalytic use of a composite material, RuO2/BaTi 4O9, in combination with NaIO4 in EtOAc-H 2O has been shown to efficiently cleave alkenes, affording ketones, aldehydes and/or carboxylic acids in high yields. Georg Thieme Verlag Stuttgart.

An iron-promoted aldehyde-diene cyclocoupling reaction

(Chemical Equation Presented) A stereospecific intramolecular iron tricarbonyl-promoted aldehyde-diene cyclocoupling reaction was investigated by using simple substrates 6 and more complicated substrates 30a/30b. Demetalation of the initial products conve

Piperidinyl and piperazinyl compounds substituted with bicyclo-heterocyclylalkyl groups useful as CCR3 receptor antagonists

Compounds having the Formula (I), are useful as CCR3 receptor antagonists, wherein Ar is aryl or heteroaryl; Q is —C(═O)— or C1-2alkylene; X is N(+)R9a, or N; Y is CR9b, or N; R2 is hydrogen or alkyl; R3 and R4 are as defined in the specification; Uc is a mono- or bicyclic group as defined in the specification; n is 0 or 1; and p is 0, 1, 2, 3 or 4.

4-Amido-2-carboxytetrahydroquinolines. Structure-Activity Relationships for Antagonism at the Glycine Site of the NMDA Receptor

trans-2-Carboxy-5,7-dichloro-4-amidotetrahydroquinolines, evolved from the lead 5,7-dichlorokynurenic acid, have been synthesized and tested for in vitro antagonist activity at the glycine site on the N-methyl-D-aspartate (NMDA) receptor.Optimization of the 4-substituent has provided antagonists having nanomolar affinity, including the urea trans-2-carboxy-5,7-dichloro-4-amino>-1,2,3,4-tetrahydroquinoline (35; IC50 = 7.4 nM vs glycine binding; Kb = 130 nM for block of NMDA responses in the rat cortical slice), which is one of the most poten t NMDA antagonists yet found.The absolute stereochemical requirements for binding were found to be 2S,4R, showing that, in common with other glycine-site NMDA receptor ligands, the unnatural configuration at the α-amino acid center is required.The preferred conformation of the trans-2,4-disubstituted tetrahydroquinoline system, as shown by X-ray crystallography and 1H NMR studies, places the 2-carboxyl pseudoequatorial and the 4-substituent pseudoaxial.Modifications of the 4-amide show that bulky substituents are tolerated and reveal the critical importance for activity of correct positioning of the carbonyl group.The high affinity of trans-2-carboxy-5,7-dichloro-4--1,2,3,4-tetrahydroquinoline (55; IC50 = 6 nM) suggests that the Z,Z-conformer of the phenyl urea moiety in 35 is recognized by the receptor.Molecular modeling studies show that the 4-carbonyl groups of the kynurenic acids, the tetrahydroquinolines, and related antagonists based on N-(chlorophenyl)glycine, can interact with a single putative H-bond donor on the receptor.The results allow the establishment of a three-dimensional pharma cophore of the glycine receptor antagonist site, incorporating a newly defined bulk tolerance/hydrophobic region.