- Tertiary amine compound, bisphosphine ligand, and intermediate and preparation method of tertiary amine compound
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The invention discloses a tertiary amine compound, a bisphosphine ligand, and an intermediate and a preparation method of the tertiary amine compound, and provides a tertiary amine compound preparation method, which comprises: under the protection of a ga
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Paragraph 0232; 0236-0239; 0240; 0250-0252
(2019/11/20)
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- Enantioselective Rhodium-Catalyzed Addition of Arylboroxines to N-Unprotected Ketimines: Efficient Synthesis of Cipargamin
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Highly enantioselective rhodium-catalyzed addition of arylboroxines to N-unprotected ketimines is realized for the first time by employing chiral BIBOP-type ligands with a Rh loading as low as 1 mol %. A range of chiral α-trifluoromethyl-α,α-diaryl α-tertiary amines or 3-amino-3-aryloxindoles were formed with excellent ee values and yields by employing either WingPhos or PFBO-BIBOP as the ligand. The method has enabled an efficient enantioselective synthesis of cipargamin.
- Zhu, Jinbin,Huang, Linwei,Dong, Wei,Li, Naikai,Yu, Xingxin,Deng, Wei-Ping,Tang, Wenjun
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supporting information
p. 16119 - 16123
(2019/11/03)
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- Enantioselective Friedel–Crafts Alkylation Reaction of Heteroarenes with N-Unprotected Trifluoromethyl Ketimines by Means of Chiral Phosphoric Acid
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An enantioselective Friedel–Crafts alkylation reaction of pyrroles and indoles with N-unprotected trifluoromethyl ketimines by use of chiral phosphoric acid provided α-trifluoromethylated primary amines bearing chiral tetrasubstituted carbon centers in high yields and with high to excellent enantioselectivities. The present reaction is unique to N-unprotected trifluoromethyl ketimines. No reaction took place with N-p-methoxyphenyl (PMP)-substituted ketimine. Corresponding α-trifluoromethylated amines were transformed without loss of enantioselectivity.
- Miyagawa, Masamichi,Yoshida, Masaru,Kiyota, Yuki,Akiyama, Takahiko
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supporting information
p. 5677 - 5681
(2019/04/03)
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- REVERSIBLE INHIBITORS OF MONOAMINE OXIDASE A AND B
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The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.
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Page/Page column 39-40
(2008/06/13)
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- Unprecedented catalytic asymmetric reduction of N-H imines
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(Chemical Equation Presented) Addition of lithium bis(trimethylsilyl)amide to perfluorinated ketones 1a-j affords (E)-N-TMS-ketimines 2a-j that are reduced in situ to afford racemic perfluoromethylated amine hydrochloride salts 3a-j in 54-97% yields. Solv
- Gosselin, Francis,O'Shea, Paul D.,Roy, Stephanie,Reamer, Robert A.,Chen, Cheng-Yi,Volante, Ralph P.
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p. 355 - 358
(2007/10/03)
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