Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Atsuko Nishiguchi"'
Publikováno v:
Tetrahedron. 74:5779-5790
A practical chromatography-free synthesis of a potent polo-like kinase-1 inhibitor possessing a unique 5,6-dihydroimidazolo[1,5-f]pteridine structure has been developed. We showed that key cyanoimidazole ring formation could be conducted at benign te
Phosphine-Catalyzed Enantioselective Intramolecular [3+2] Annulations To Generate Fused Ring Systems
Publikováno v:
Journal of the American Chemical Society
Substantial progress has been described in the development of asymmetric variants of the phosphine-catalyzed intermolecular [3+2] annulation of allenes with alkenes; however, there have not been corresponding advances for the intramolecular process,
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:
ChemInform. 46
A simple protocol employing the chiral phosphine catalysts (I) is presented for the synthesis of diquinane, fused pyrrolidine, coumarine, and quinoline derivatives.
Publikováno v:
Tetrahedron. 61:5043-5048
The sulfide 4 was treated with chiral acid in a mixture of toluene and methyl iso -butylketone to precipitate the salt, which reacted with 30% H 2 O 2 for 3 weeks at rt. The resulting crystals were collected followed by recrystallization to give the
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, 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
Publikováno v:
The Journal of Organic Chemistry. 65:6922-6931
A combination of sulfanyl radical addition-cyclization of dienes connected with hydroximates and subsequent conversion of the resulting cyclic hydroximate to the lactones provides a novel method for the construction of alpha,beta-disubstituted gamma-