反応 #43278

ord-9bb50b18badf4dd7903ca55bbb1fedd2

反応方程式

CCOC(=O)Cc1ccc2c(c1)N(C(=O)OC(C)(C)C)c1ccccc1S2(=O)=O
tert-butyl 2-ethoxycarbonylmethyl-5,5-dioxo-5H-phenothiazine-10-carboxylate
FC1(F)CCC(CI)CC1
1,1-difluoro-4-iodomethylcyclohexane
CCOC(=O)C1CCC(F)(F)CC1
ethyl 4,4-difluorocyclohexanecarboxylate
[I-]
iodide
Cn1ccc(N)n1
1-methyl-1H-pyrazol-3-amine
Cn1ccc(NC(=O)C(CC2CCC(F)(F)CC2)c2ccc3c(c2)Nc2ccccc2S3(=O)=O)n1
3-(4,4-difluorocyclohexyl)-2-(5,5-dioxo-5,10-dihydrophenothiazin-2-yl)-N-(1-methyl-1H-pyrazol-3-yl)propionamide

反応条件

詳細条件
See reaction.notes.procedure_details.

実験手順

Analogously to Example 36 and Example 44, tert-butyl 2-ethoxycarbonylmethyl-5,5-dioxo-5H-phenothiazine-10-carboxylate, 1,1-difluoro-4-iodomethylcyclohexane (prepared from commercially available ethyl 4,4-difluorocyclohexanecarboxylate analogously to the synthesis of the iodide described in Example 40) and 1-methyl-1H-pyrazol-3-amine give 3-(4,4-difluorocyclohexyl)-2-(5,5-dioxo-5,10-dihydrophenothiazin-2-yl)-N-(1-methyl-1H-pyrazol-3-yl)propionamide.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07732440B2uspto-grants-2010_06