189059-58-3

Usage

Uses

An intermediate of Lapaquistat acetate (L175500).

Upstream product

• 152911-43-8 (2-amino-5-chlorophenyl)(2,3-dimethoxyphenyl)methanone 
• 177410-67-2 (+/-)-5-chloro-α-(2,3-dimethoxyphenyl)-2-pivaloylaminobenzyl acetate 
• 177410-73-0 (+/-)-5-chloro-α-(2,3-dimethoxyphenyl)-2-pivaloylaminobenzyl alcohol 
• 152911-54-1 (+/-)-2-amino-5-chloro-α-(2,3-dimethoxyphenyl)benzyl alcohol 
• 177410-76-3 (S)-(-)-5-chloro-α-(2,3-dimethoxyphenyl)-2-pivaloylaminobenzyl alcohol 

Downstream Products

• 177410-77-4 (S)-[5-Chloro-2-(2,2-dimethyl-propylamino)-phenyl]-(2,3-dimethoxy-phenyl)-methanol 
• 189059-60-7 (S)-5-chloro-α-(2,3-dimethoxyphenyl)-2-(3-hydroxy-2,2-dimethylpropyl)aminobenzyl alcohol 
• 177567-44-1 (E)-3-[{4-Chloro-2-[(S)-(2,3-dimethoxy-phenyl)-hydroxy-methyl]-phenyl}-(2,2-dimethyl-propyl)-carbamoyl]-acrylic acid ethyl ester 
• 177567-40-7 [(3R,5S)-7-Chloro-5-(2,3-dimethoxy-phenyl)-1-(2,2-dimethyl-propyl)-2-oxo-1,2,3,5-tetrahydro-benzo[e][1,4]oxazepin-3-yl]-acetic acid ethyl ester 
• 171868-39-6 (3R,5S)-(-)-(3,5-trans)-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-1-neopentyl-2-oxo-4,1-benzoxazepine-3-acetic acid 
• 473987-24-5 benzyl 1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-[2,2-dimethyl-3-(pivaloyloxymethyloxy)propyl]-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-acetate 
• 473987-22-3 benzyl 1-[[(3R,5S)-1-[3-(butyryloxy)-2,2-dimethylpropyl]-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-acetate 
• 473987-21-2 benzyl 1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-[2,2-dimethyl-3-(propionyloxy)propyl]-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-acetate 
• 473987-23-4 benzyl 1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-[2,2-dimethyl-3-(isobutyryloxy)propyl]-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-acetate 
• 473987-20-1 benzyl 1-[[(3R,5S)-7-chloro-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-1,2,3,5-tetrahydro-5-(2,3-dimethoxyphenyl)-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-acetate 
• 473987-14-3 ethyl 1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-butyrate 
• 473987-13-2 ethyl 1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-propionate 
• 189060-13-7 (1-{2-[(3R,5S)-1-(3-Acetoxy-2,2-dimethyl-propyl)-7-chloro-5-(2,3-dimethoxy-phenyl)-2-oxo-1,2,3,5-tetrahydro-benzo[e][1,4]oxazepin-3-yl]-acetyl}-piperidin-4-yl)-acetic acid 
• 189059-65-2 ethyl 1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl]piperidine-4-acetate 

Relevant academic research and scientific papers

A chiral bimetallic Lewis acid as a reaction template. Asymmetric reduction of unsymmetric ketones with LiBH4

A new series of chiral bimetallic Lewis acids, 5,5'-bis[(R)-2-aryl- 1,3,2-dioxaborolan-4-one], have been prepared from L-(+)-tartaric acid and arylboronic acids. In the presence of these Lewis acids, unsymmetric ketones were reduced quantitatively by LiBH

Process research on the asymmetric hydrogenation of a benzophenone for developing the manufacturing process of the squalene synthase inhibitor TAK-475

A practical synthetic method for the synthesis of the chiral benzhydrol 8, which is the key intermediate of the squalene synthase inhibitor TAK-475 (1), has been developed. The method, via asymmetric hydrogenation of the benzophenone 7, employed Noyori's ruthenium precatalyst of the type [RuCl 2(diphosphine)(diamine). We focused on tuning of the chiral diphosphine, and have discovered a novel ligand, DADMP-BINAP (18c), for the catalyst that has allowed reduction of the operating pressure in the asymmetric hydrogenation. The precatalyst containing 18c performed effectively at low hydrogen pressure (1 MPa) with sufficient enantioselectivity, and the result enabled us to successfully obtain enantiomerically pure 8 on a multikilogram scale.

DIPHOSPHINE LIGAND AND TRANSITION METAL COMPLEX USING THE SAME

The present invention provides a novel ligand represented by the following formula and a novel transition metal complex having the ligand, which shows superior enantioselectivity and catalytic efficiency, particularly high catalyst activity, in various asymmetric synthesis reactions. A transition metal complex having, as a ligand, a compound represented by the formula wherein R4 is a hydrogen atom or a C1-6 alkyl group optionally having substituent(s), and R5 and R6 are each a C1-6 alkyl group optionally having substituent(s), or the formula is a group represented by the formula wherein ring B is a 3- to 8-membered ring optionally having substituent (s).

HIGHLY SELECTIVE NOVEL AMIDATION METHOD

The present invention provides an industrial production method with a short process having a high yield of an aliphatic cyclic carboxamide having carboxyl group, which comprises reacting functional group-selectively using an inexpensive condensing agen

Microbial enantioselective ester hydrolysis for the preparation of optically active 4,1-benzoxazepine-3-acetic acid derivatives as squalene synthase inhibitors

Microbial enantioselective ester hydrolysis for the preparation of optically active (3R,5S)-(-)-5-phenyl-4,1-benzoxazepine-3-acetic acid derivatives as potent squalene synthase inhibitors was investigated. Pseudomonas diminuta and Pseudomonas taetrolens h