51326-00-2Relevant articles and documents
Copper-Catalyzed Enantioselective 1,2-Reduction of Cycloalkenones
Shi, Yongjie,Wang, Jingxin,Yin, Qin,Zhang, Xumu,Chiu, Pauline
supporting information, p. 5658 - 5663 (2021/08/01)
We report an asymmetric 1,2-reduction of cyclic α,β-unsaturated ketones to access various enantiomerically enriched cyclic allylic alcohols under mild conditions, catalyzed by in situ generated copper hydride ligated with (R)-DTBM-C3*-TunePhos. α-Brominated cycloalkenones were reduced with excellent enantioselectivities of up to 98% ee, while substrates that were without α-substituents were reduced chemoselectively, with moderate enantioselectivities.
N-(1-(METHYLSULFONYL)PIPERIDIN-4-YL)-4,5-DI HYDRO-1H-IMIDAZO[4,5-H]QUINAZOLIN-8-AMINE DERIVATIVES AND RELATED COMPOUNDS AS CYCLIN-DEPENDENT KINASE 2 (CDK2) INHIBITORS FOR TREATING CANCER
-
Page/Page column 130, (2020/11/13)
The present application provid es tricyclic amine compounds of formula (I) as inhibitors of cyclin-dependent kinase 2 (CDK2) for treating cancer. Preferred compounds are N-(1-(methylsulfonyl)piperidin-4- yl)-4,5-dihydro-lH-imidazo[4,5-h]quinazolin-8-amine and the corresponding 6,8-dihydro-5H-pyrazolo[3,4-h]quinazolin-2-amine, 6,8- dihydropyrazolo[4',3':4,5]pyrano[3,2-d]pyrimidin-2-amine and 1,4- dihydroimidazo[4',5': 4,5]pyrano[3,2-d]pyrimidin-8-amine derivatives of formulae (IVa) to (IVd). The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 128 to 166; examples 1 to 32, A and B1 to B10; table 1). Exemplary compound are e.g.: N-(1-(ethylsulfonyl)piperidin-4-yl)-l,2-dimethyl-4,5-dihydro-1H- imidazo[4,5-h]quinazolin-8-amine (example 1) 8-Methyl-N-(1-(methylsulfonyl)piperidin-4-yl)-6,8-dihydro-5H- pyrazolo[3,4-h]quinazolin-2-amine (example 9) 8-Methyl-N-(1-(methylsulfonyl)piperidin-4-yl)-6,8- dihydropyrazolo[4',3':4,5]pyrano[3,2-d]pyrimidin-2-amine (example 10) 1-cyclopropyl-N-(1-(methylsulfonyl)piperidin-4-yl)-l,4- dihydroimidazo[4',5':4,5]pyrano [3,2-d]pyrimidin-8-amine (example 26).
Efficient Synthesis of Anastrephin via the Allylic Substitution for Quaternary Carbon Construction
Wada, Kyohei,Sakai, Masahiro,Kawashima, Hidehisa,Ogawa, Narihito,Kobayashi, Yuichi
supporting information, p. 1428 - 1432 (2016/05/24)
Lactone-moiety-attached 2-cyclohexylideneethyl picolinate was prepared through the OH-directed epoxidation (98% ds) of (R)-3-methylcyclohex-2-en-1-ol (99% ee), Horner-Wadsworth-Emmons olefination, conversion to the allylic moiety, and epoxide ring opening