- An entry to 2-(cyclobut-1-en-1-yl)-1: H -indoles through a cyclobutenylation/deprotection cascade
-
A transition-metal-free strategy for the synthesis of 2-(cyclobut-1-en-1-yl)-1H-indoles under mild conditions is described herein. A series of substituted 2-(cyclobut-1-en-1-yl)-1H-indoles are accessed by a one-pot cyclobutenylation/deprotection cascade from N-Boc protected indoles. Preliminary experimental and density functional theory calculations suggest that a Boc-group transfer is involved in the underlying mechanism.
- Natho, Philipp,Yang, Zeyu,Allen, Lewis A. T.,Rey, Juliette,White, Andrew J. P.,Parsons, Philip J.
-
supporting information
p. 4048 - 4053
(2021/05/19)
-
- Three-Component Reaction for the Synthesis of Highly Functionalized Propargyl Ethers
-
Multicomponent reactions provide efficient means to access molecular complexity. Herein, we report a copper-catalyzed three-component reaction of diazo compounds, alcohols and ethynyl benziodoxole (EBX) reagents for the synthesis of propargyl ethers. Extensive variations of the three partners of the reaction is possible, leading to highly functionalized and structurally diverse products under mild conditions. Alkynylation of a copper ylide intermediate is postulated as key step for this transformation.
- Pisella, Guillaume,Gagnebin, Alec,Waser, Jér?me
-
supporting information
p. 10199 - 10204
(2020/07/17)
-
- Synthesis of 3-fluoromethyl-2,1-benzisoxazoles
-
A convenient synthetic method to access hitherto unknown 3-(trifluoromethyl)- and 3-(difluoromethyl)-2,1-benzisoxazoles by the reaction of sodium azide with 1-(2-halophenyl)-2,2,2-trifluoroethanones or 1-(2-halophenyl)-2,2-difluoroethanones was developed. 3-Fluoromethyl-2,1-benzisoxazoles are versatile precursors for o-fluoroacetylanilines.
- Golubev,Shidlovskii,Peregudov,Kagramanov
-
p. 2264 - 2270
(2015/06/22)
-
- PROCESS FOR PREPARING EFAVIRENZ
-
The invention disclosed a 4 step process for the preparation of Efavirenz, starting from 1,4-dichlorobenzene, and its intermediates.
- -
-
Page/Page column 34
(2012/06/30)
-
- DMP-266 BY CYCLISATION
-
Disclosed is a method for the preparation of the HIV drug Efavirenz, also known as DMP-266, starting from 1,4-dichlorobenzene, and its intermediates.
- -
-
Page/Page column 57
(2012/08/07)
-
- PROCESS FOR PREPARATION OF EFAVIRENZ BY CYCLISATION
-
The invention disclosed a process for the preparation of the HIV drug Efavirenz, also known as DMP-266, starting from 1,4-dichlorobenzene, and its intermediates.
- -
-
Page/Page column 56
(2012/08/07)
-
