- Liquid chromatography enantiomeric separation of chiral ethanolamine substituted compounds
-
Eleven racemic ethanolamine derivatives were prepared, and their enantiomers were separated using liquid chromatography with various chiral columns. These derivatives included chiral vicinal amino alcohols, β-hydroxy ureas, β-hydroxy thioureas, and β-hydr
- Armstrong, Daniel W.,Berthod, Alain,Firooz, Sepideh Khaki,Fulton, Brandon,Lovely, Carl J.,Putman, Joshua
-
-
- Chiral-Organotin-Catalyzed Kinetic Resolution of Vicinal Amino Alcohols
-
A highly efficient kinetic resolution of racemic amino alcohols has been achieved for the first time with a chiral tin catalyst. A chiral organotin compound with 3,4,5-trifluorophenyl groups at the 3,3′-positions of the binaphthyl framework enabled this transformation with excellent yield and high enantioselectivity. The process tolerates aryl- and alkyl-substituted amino alcohols and a variety of other substrates, affording the corresponding products in high enantioselectivity and with s factors up to >500.
- Yang, Hui,Zheng, Wen-Hua
-
supporting information
p. 16177 - 16180
(2019/11/03)
-
- OXAZOLE AND THIAZOLE DERIVATIVES AS INHIBITORS OF ASK1
-
The present technology is directed to compounds of formula (I), compositions thereof, and methods related to inhibition of ASKI. In particular, the present compounds and compositions may be used to treat ASKl-mediated disorders and conditions, including,
- -
-
-
- Use of a Catalytic Chiral Leaving Group for Asymmetric Substitutions at sp3-Hybridized Carbon Atoms: Kinetic Resolution of β-Amino Alcohols by p-Methoxybenzylation
-
A catalytic strategy was developed for asymmetric substitution reactions at sp3-hybridized carbon atoms by using a chiral alkylating agent generated in situ from trichloroacetimidate and a chiral phosphoric acid. The resulting chiral p-methoxybenzyl phosphate selectively reacts with β-amino alcohols rather than those without a β-NH functionality. The use of an electronically and sterically tuned chiral phosphoric acid enables the kinetic resolution of amino alcohols through p-methoxybenzylation with good enantioselectivity.
- Kuroda, Yusuke,Harada, Shingo,Oonishi, Akinori,Kiyama, Hiroki,Yamaoka, Yousuke,Yamada, Ken-Ichi,Takasu, Kiyosei
-
supporting information
p. 13137 - 13141
(2016/10/30)
-
- Kinetic resolution of racemic amino alcohols through intermolecular acetalization catalyzed by a chiral Bronsted acid
-
The kinetic resolution of racemic secondary alcohols is a fundamental method for obtaining enantiomerically enriched alcohols. Compared to esterification, which is a well-established method for this purpose, kinetic resolution through enantioselective intermolecular acetalization has not been reported to date despite the fact that the formation of acetals is widely adopted to protect hydroxy groups. By taking advantage of the thermodynamics of acetalization by the addition of alcohols to enol ethers, a highly efficient kinetic resolution of racemic amino alcohols was achieved for the first time and in a practical manner using a chiral phosphoric acid catalyst.
- Yamanaka, Takuto,Kondoh, Azusa,Terada, Masahiro
-
supporting information
p. 1048 - 1051
(2015/02/19)
-
- PYRIDO PYRIMIDINES
-
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
- -
-
-
- ANTI VIRAL COMPOUNDS
-
There is provided small molecule anti-human immunodeficiency virus (anti-HIV) compounds as well as a phenotypic cell-based high throughput screening (HTS) assay for their identification.
- -
-
Page/Page column 156-157
(2010/05/13)
-
- Asymmetric oxidations of electron-poor alkenes promoted by the β-amino alcohol/TBHP system
-
The asymmetric oxyfunctionalization of alkenes is a fundamental process in synthetic organic chemistry. In this contribution, we review our findings on the enantioselective organocatalyzed oxidation of electron-poor alkenes. Readily or commercially available β-amino alcohols displayed catalytic activity in the asymmetric epoxidation of α,β-enones and β-peroxidation of nitroalkenes with tert-butyl hydroperoxide (TBHP) as the oxidant. The corresponding epoxides and peroxides were isolated in good to high yield and enantioselectivity. Georg Thieme Verlag Stuttgart.
- Russo, Alessio,Lattanzi, Alessandra
-
scheme or table
p. 1551 - 1556
(2009/12/06)
-
- INHIBITORS OF AKT ACTIVITY
-
Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
- -
-
Page/Page column 113
(2008/06/13)
-
- 1,4-benzodioxin derivatives
-
PCT No. PCT/JP96/01252 Sec. 371 Date Nov. 12, 1997 Sec. 102(e) Date Nov. 12, 1997 PCT Filed May 13, 1996 PCT Pub. No. WO96/35685 PCT Pub. Date Nov. 14, 1996A 1,4-benzodioxin derivative represented by formula (I) wherein A is an aryl group or a (C3-C8)cycloalkyl group, R1 and R2 individually are a hydrogen atom, a halogen atom, an alkyl group, a trifluoromethyl group, an alkoxy group, an aryl group, an aryloxy group, or R1 and R2 together form a methylenedioxy group, R3 is a hydrogen atom or an alkyl group, R4 is a hydrogen atom or CO2R5, R5 is a hydrogen atom or an alkyl group, X is a radical of formula (II) or (III) wherein n is 1 or 2. The compounds are useful for a prophylactic or therapeutic agent for diabetes, hyperglycemia and obesity.
- -
-
-
- The aluminum amalgam reduction of 2-nitroalkanols promoted by ultrasound
-
The sonochemical promoted aluminum amalgam reduction of 2-nitroalkanols provides an improved yield and accelerated conversion to the corresponding amino alcohols when compared to the nonultrasound (benchtop) reductions. The appearance of by-product hydrox
- Fitch, Richard W.,Luzzio, Frederick A.
-
p. 6013 - 6016
(2007/10/02)
-