51690-50-7

Upstream product

• 10321-71-8 4-methyl-pent-2-enoic acid 
• 71-43-2 benzene 
• 72277-17-9 (+/-)-ethyl 4-methyl-3-phenylpentanoate 
• 77921-03-0 (E)-4-methyl-3-phenyl-2-pentenoic acid 
• 920-39-8 isopropylmagnesium bromide 
• 621-82-9 Cinnamic acid 
• 57361-18-9 2-(N-Cyclohexyl-N-methylamino)-5-methyl-4-phenyl-2-hexennitril 
• 100613-11-4 (2-methyl-1-phenyl-propyl)-malonic acid 
• 140-10-3 (E)-3-phenylacrylic acid 
• 1068-55-9 isopropylmagnesium chloride 
• 14371-10-9 (E)-3-phenylpropenal 
• 611-70-1 phenyl isopropyl ketone 
• 104290-61-1 2-Chloro-3,3-dimethyl-2-phenyl-cyclopropanecarboxylic acid methyl ester 
• 4460-46-2 3-chloro-3-phenyl-3H-diazirine 

Downstream Products

• 22573-54-2 (R)-3-phenyl-4-methylpentanoic acid 
• 72277-17-9 (+/-)-ethyl 4-methyl-3-phenylpentanoate 
• 126275-15-8 4-methyl-3-phenylpentanoyl chloride 
• 1019003-37-2 (R)-ethyl 4-methyl-3-phenylpentanoate 
• 22573-51-9 (S)-(-)-3-phenyl-4-methylpentanoic acid 
• 1462940-80-2 (R)-2,3,5,6-tetrafluoro-4-methylbenzyl 4-methyl-3-phenylpentanoate 
• 1462940-81-3 (S)-2,3,5,6-tetrafluoro-4-methylbenzyl 4-methyl-3-phenylpentanoate 
• 20894-20-6 5,5-dimethyl-4-phenylpyrrolidin-2-one 
• 55001-06-4 acid γ-isopropyl γ-phenyl butirique 
• 55001-05-3 [1-(2-Bromo-ethyl)-2-methyl-propyl]-benzene 
• 126275-02-3 (+/-) α-(RS)-Cyano-3-phenoxybenzyl-4-methyl-3-phenylpentanoate 
• 83303-62-2 1-Diazo-5-methyl-4-phenyl-hexan-2-one 
• 199468-80-9 (S)-3-((2R,3S)-2-Azido-4-methyl-3-phenyl-pentanoyl)-4-phenyl-oxazolidin-2-one 
• 175853-65-3 (R)-3-((2S,3R)-2-Azido-4-methyl-3-phenyl-pentanoyl)-4-phenyl-oxazolidin-2-one 

Relevant academic research and scientific papers

Ruthenium-catalyzed intramolecular arene C(sp2)-H amidation for synthesis of 3,4-dihydroquinolin-2(1 H)-ones

We report the [Ru(p-cymene)(l-proline)Cl] ([Ru1])-catalyzed cyclization of 1,4,2-dioxazol-5-ones to form dihydroquinoline-2-ones in excellent yields with excellent regioselectivity via a formal intramolecular arene C(sp2)-H amidation. The reactions of the 2- and 4-substituted aryl dioxazolones proceeds initially through spirolactamization via electrophilic amidation at the arene site, which is para or ortho to the substituent. A Hammett correlation study showed that the spirolactamization is likely to occur by electrophilic nitrenoid attack at the arene, which is characterized by a negative ρ value of -0.73.

Quantitative Analysis on Two-Point Ligand Modulation of Iridium Catalysts for Chemodivergent C-H Amidation

The transition-metal-catalyzed nitrenoid transfer reaction is one of the most attractive methods for installing a new C-N bond into diverse reactive units. While numerous selective aminations are known, understanding complex structural effects of the key intermediates on the observed chemoselectivity is still elusive in most cases. Herein, we report a designing approach to enable selective nitrenoid transfer leading to sp2 spirocyclization and sp3 C-H insertion by cooperative two-point modulation of ligands in the CpXIr(III)(κ2-chelate) catalyst system. Computational analysis led us to interrogate structural motifs that can be attributed to the desired mechanistic dichotomy. Multivariate linear regression analysis on the perturbation on the η5-cyclopentadienyl ancillary (CpX) and LX coligand, wherein we prepared over than 40 new catalysts for screening, allowed for construction of an intuitive yet robust statistical model that predicts a large set of chemoselective outcomes, implying that the catalysts' structural effects play a critical role on the chemoselective nitrenoid transfer. On the basis of this quantitative analysis, a new catalytic platform is now established for the unique lactam formation, leading to the unprecedented chemoselective reactivity (up to >20:1) toward a diverse array of competing sites, such as tertiary, secondary, benzylic, allylic C-H bonds, and aromatic πsystem.

Construction of enantioenriched 9H-Fluorene frameworks via a cascade reaction involving remote vinylogous dynamic kinetic resolution

The benzylic C-H group of α,α-dicyanoolefins from 3-substituted 1-indanones could be significantly activated via transmission along the aromatic system, thus enabling dynamic kinetic resolution via a traditional reversible deprotonation- protonation process. Enantioenriched 9-substituted 9H-fluorene frameworks were finally constructed through an asymmetric vinylogous Michael addition to nitroolefins, followed by a cascade cyclization and oxidative aromatization process, under the catalysis of a chiral bifunctional thiourea-tertiary amine.

Identification of an Esterase Isolated Using Metagenomic Technology which Displays an Unusual Substrate Scope and its Characterisation as an Enantioselective Biocatalyst

Evaluation of an esterase annotated as 26D isolated from a marine metagenomic library is described. Esterase 26D was found to have a unique substrate scope, including synthetic transformations which could not be readily effected in a synthetically useful manner using commercially available enzymes. Esterase 26D was more selective towards substrates which had larger, more sterically demanding substituents (i. e. iso-propyl or tert-butyl groups) on the β-carbon, which is in contrast to previously tested commercially available enzymes which displayed a preference for substrates with sterically less demanding substituents (e.g. methyl group) at the β-carbon. (Figure presented.).

Stereoselective Sulfinyl Aniline-Promoted Pd-Catalyzed C?H Arylation and Acetoxylation of Aliphatic Amides

Stereoselective functionalization of aliphatic C?H bonds presents a great challenge. Following this target, we disclose herein an original strategy towards direct arylation of aliphatic chains at ?-methylene position based on a use of amide-sulfoxide bicoordinating directing group. Although moderate to high chiral induction (up to 9:1 d.r.) is achieved, diastereomerically pure compounds may be afforded by simple separation of diastereomeric products by silica gel chromatography. Accordingly, this reaction allows preparation of a large scope of high-value scaffolds in synthetically useful yields while recyclable character of our chiral auxiliary brings an additional benefit. A potential of this methodology to build up original molecules by sequential diarylation and expedient (two step) synthesis of a biologically active compound are further disclosed. Finally a first example of stereoselective direct acetoxylation of aliphatic chains is reported.

Direct β-Selective Hydrocarboxylation of Styrenes with CO2 Enabled by Continuous Flow Photoredox Catalysis

The direct β-selective hydrocarboxylation of styrenes under atmospheric pressure of CO2 has been developed using photoredox catalysis in continuous flow. The scope of this methodology was demonstrated with a range of functionalized terminal styrenes, as well as α-substituted and β-substituted styrenes.

Lipase catalysed kinetic resolutions of 3-aryl alkanoic acids

Hydrolase catalysed kinetic resolutions leading to a series of 3-aryl alkanoic acids (≥94% ee) are described. Hydrolysis of the ethyl esters with a series of hydrolases was undertaken to identify biocatalysts that yield the corresponding acids with excellent enantiopurity in each case. Steric and electronic effects on the efficiency and enantioselectivity of the biocatalytic transformation were also explored.

Lipase catalyzed acylation of primary alcohols with remotely located stereogenic centres: the resolution of (±)-4,4-dimethyl-3-phenyl-1-pentanol

Enantioselective acylation of some (±)-3-alkyl-3-phenyl-1-propanols was performed with enzymes as catalysts. Moderate enantiomeric ratios (E), ranging up to E = 11.6, were obtained. In the resolution, some of the lipases selectively acylated the (+)-enant

NITROGENOUS CYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

The present invention provides a novel compound having a superior calcium antagonism, in particular, a neuron-selective calcium antagonism. Namely, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, Ar indicates an optionally substituted 5- to 14-membered aromatic ring etc.; the ring A indicates any one ring selected from a piperazine, a homopiperazine, a piperidine and the like; the ring B indicates an optionally substituted C3-14 hydrocarbon ring etc.; E indicates a single bond, a group represented by the formula -CO-, etc.; X indicates a single bond, an oxygen atom etc.; R1 indicates a hydrogen atom, a halogen atom, a hydroxyl group etc.; and D1, D2, W1 and W2 are the same as or different from each other and each represents a single bond or an optionally substituted C1-6 alkylene chain.

Enantioselective conjugate radical addition reactions mediated by chiral Lewis acid complexes of (R,R)-4,6-dibenzofurandiyl-2,2'-bis(4- phenyloxazoline) (DBFOX/Ph)

A high-yielding synthesis (50% overall yield) of tridentate bisoxazoline ligand (R,R)-4,6-dibenzofurandiyl-2,2'-bis(4-phenyloxazoline) (DBFOX/Ph) was developed. DBFOX/Ph was subsequently tested in enantioselective conjugate radical additions onto 3-(3-phe