Zobrazeno 1 - 10
of 34
pro vyhledávání: '"Kiminori Tomimatsu"'
Publikováno v:
Tetrahedron. 63:4048-4051
A convenient synthesis method of antisepsis agent TAK-242 ((R)-1) through diastereomeric resolution was developed. By condensation of racemate rac-1 with chiral acid (S)-O-acetylmanderic acid (6a), the desired diastereomer 5a was isolated with 98% de
Publikováno v:
Organic Process Research & Development. 9:168-173
A practical method of synthesizing 7-{4-[2-(butoxy)ethoxy]phenyl}-N-(4-{[methyl(tetrahydro-2H-pyran-4-yl)amino]methyl}phenyl)-1-propyl-2,3-dihydro-1H-1-benzazepine-4-carboxamide (8), an orally active CCR5 antagonist, has been developed. Methyl 7-brom
Publikováno v:
Tetrahedron Letters. 45:9335-9339
A convenient large-scalable synthesis of 1-benzazepines 19 as an important intermediate of CCR5 antagonist, oral HIV-1 therapy, was established. The anilination of o -halogenobenzaldehyde 9 with alkylamino-acid 16 gave o -formylaniline-acid 17 . Comp
Autor:
Kiminori Tomimatsu, Mitsuhisa Yamano, Tatsuya Ito, Tomomi Ikemoto, Toshiaki Nagata, Yukio Mizuno
Publikováno v:
Tetrahedron Letters. 45:7757-7760
An asymmetric synthesis of (R)-(+)-6-(1,4-dimethoxy-3-methyl-2-naphthyl)-6-(4-hydroxyphenyl)hexanoic acid 2 as a key intermediate for a neurodegenerative disease agent 1 has been developed. A key reaction was an asymmetric hydrogenation of hindered a
Publikováno v:
Tetrahedron: Asymmetry. 14:3525-3531
A practical method for the preparation of ( R )-(+)-6-(1,4-dimethoxy-3-methyl-2-naphthyl)-6-(4-hydroxyphenyl)hexanoic acid ( R )- 2 , a key intermediate for a therapeutic drug for neurodegenerative diseases, has been developed. rac -Methyl 6-(1,4-dim
Autor:
Kiminori Tomimatsu, Tatsuya Ito, Yasushi Isogami, Toru Ishida, Hiroki Wada, Yukio Mizuno, Kazumasa Hamamura, Tetsuji Kawamoto, Yoshiko Miyano, Tomomi Ikemoto, Muneo Takatani, Mitsuhiro Wakimasu
Publikováno v:
Tetrahedron. 58:489-493
The 5-thia-1,8b-diazaacenaphthylenes ( 2 and its ester, 8 ) are new cyclazines, in which a paramagnetic ring is present in the peripheral 12π-electron ring system. Three convenient methods of preparing 8 have been developed. One involved thioglycola
Autor:
Tadashi Hanaoka, Hideaki Maruyama, Tatsuya Itoh, Hideo Hashimoto, Mitsuhiro Wakimasu, Tomomi Ikemoto, Kiminori Tomimatsu, and Hiroyuki Mitsudera
Publikováno v:
Organic Process Research & Development. 6:70-73
A new and efficient synthesis of 4-[N-methyl-N-(tetrahydropyran-4-yl)aminomethyl]aniline dihydrochloride, a key intermediate for the CCR5 antagonist TAK-779, is described. Reductive alkylation of methylamine with tetrahydro-4H-pyran-4-one followed by
Autor:
Kiminori Tomimatsu, Mitsuhiro Wakimasu, Atsuko Nishiguchi, Hiroyuki Mitsudera, Tomomi Ikemoto
Publikováno v:
Tetrahedron. 57:1525-1529
A convenient and efficient synthesis of TAK-779 (1a), a nonpeptide CCR5 antagonist, has been achieved. The new methylation of tertiary amine (2) using trimethyl phosphite and N-chlorosuccinimide, followed by the addition of HCl led to ammonium chlori
Autor:
Atsuko Nishiguchi, and Mitsuhiro Wakimasu, Hiroyuki Mitsudera, Kiminori Tomimatsu, Hideo Hashimoto, Tadao Kawarasaki, Tomomi Ikemoto, Tatsuya Ito
Publikováno v:
Organic Process Research & Development. 4:520-525
A new large-scalable preparation of TAK-779 (1), a non-peptide CCR5 antagonist, has been developed. The route selection was focused on in the process research. The selective reduction of commercially available benzonitrile derivative (4) as the start
Autor:
Kazumasa Hamamura, Muneo Takatani, Kiminori Tomimatsu, Hidenori Abe, Tomomi Ikemoto, Tetsuji Kawamoto
Publikováno v:
Tetrahedron Letters. 41:3447-3451
Novel 5-thia-1-azacycl[3.3.2]azine derivatives 1 , 5-thia-1,8b-diazaacenaphthylenes, have successfully been prepared. An X-ray crystallographic analysis of 1c revealed that the 5-thia-1-azacycl[3.3.2]azine ring system adopts a planar structure as to