- COMPOUNDS, COMPOSITIONS, AND METHODS OF USE
-
Described herein are compounds that act as CYP46A1 inhibitors, compositions comprising these compounds, and methods of their use into treating neurodegenerative diseases and the like, or a pharmaceutically active salt thereof. The present invention relates to compounds represented by the formula wherein each symbol is as defined in the specification, or a pharmaceutically active salt thereof.
- -
-
Paragraph 0345
(2020/12/11)
-
- Stereoselective amination of racemic sec-alcohols through sequential application of laccases and transaminases
-
A one-pot/two-step bienzymatic asymmetric amination of secondary alcohols is disclosed. The approach is based on a sequential strategy involving the use of a laccase/TEMPO catalytic system for the oxidation of alcohols into ketone intermediates, and their following transformation into optically enriched amines by using transaminases. Individual optimizations of the oxidation and biotransamination reactions have been carried out, studying later their applicability in a concurrent process. Therefore, 17 racemic (hetero) aromatic sec-alcohols with different substitutions in the aromatic ring have been converted into enantioenriched amines with good to excellent selectivities (90-99% ee) and conversion values (67-99%). The scalability of the process was also demonstrated when two different amine donors were used in the transamination step, such as isopropylamine and cis-2-buten-1,4-diamine. Satisfyingly, both sacrificial amine donors can shift the equilibrium toward the amine formation, leading to the corresponding isolated enantioenriched amines with good to excellent results.
- Martínez-Montero, Lía,Gotor, Vicente,Gotor-Fernández, Vicente,Lavandera, Iván
-
supporting information
p. 474 - 480
(2017/06/23)
-
- Chemoselective reduction of the carbonyl functionality through hydrosilylation: Integrating click catalysis with hydrosilylation in one pot
-
Herein we report the chemoselective reduction of the carbonyl functionality via hydrosilylation using a copper(I) catalyst bearing the abnormal N-heterocyclic carbene 1 with low (0.25 mol %) catalyst loading at ambient temperature in excellent yield within a very short reaction time. The hydrosilylation reaction of α,β-unsaturated carbonyl compounds takes place selectively toward 1,2-addition (C=O) to yield the corresponding allyl alcohols in good yields. Moreover, when two reducible functional groups such as imine and ketone groups are present in the same molecule, this catalyst selectively reduces the ketone functionality. Further, 1 was used in a consecutive fashion by combining the Huisgen cycloaddition and hydrosilylation reactions in one pot, yielding a range of functionalized triazole substituted alcohols in excellent yields.
- Roy, Sudipta Raha,Sau, Samaresh Chandra,Mandal, Swadhin K.
-
p. 9150 - 9160
(2014/12/11)
-
- Photocatalytic hydrogenation of acetophenone derivatives and diaryl ketones on polycrystalline titanium dioxide
-
In the absence of molecular oxygen, various aromatic ketones such as acetophenone derivatives and diaryl ketones were photocatalytically hydrogenated on polycrystalline titanium dioxide (Degussa P25) under UV light irradiation (> 340 nm). The desired secondary alcohols were obtained with excellent chemical efficiency (almost 100% yields for 10 examples) by choosing ethanol as a sacrificial hole scavenger, which was oxidized into acetaldehyde.
- Kohtani, Shigeru,Yoshioka, Eito,Saito, Kenji,Kudo, Akihiko,Miyabe, Hideto
-
experimental part
p. 1049 - 1053
(2010/11/24)
-
- ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS
-
Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
- -
-
Page/Page column 27
(2010/06/22)
-
- Aralkyltriazole compounds
-
1-phenyl-lower alkyl-1H-1,2,3-triazole compounds of the formula STR1 in which Ph represents phenyl substituted by up to and including 3 substituents selected from lower alkyl, halogen and trifluoromethyl, alk represents lower alkylidene, and wherein either R1 represents hydrogen, lower alkyl, lower alkoxy, amino, N-lower alkylamino, N,N-di-lower alkylamino, N-lower alkanoylamino, carbamoyl, N-lower alkanoylcarbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl and R2 represents carbamoyl, N-lower alkanoylcarbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl or R1 represents carbamoyl, N-lower alkanoylcarbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl and R2 represents hydrogen or lower alkyl, have anti-convulsive properties and can be used as medicaments.
- -
-
-
- 2-Ethylsulfonyl pyridine 1-oxide derivatives
-
Superior herbicidal compounds are provided having the formula: STR1 wherein X and X' are the same or different and are selected from the group consisting of chloro and fluoro.
- -
-
-