* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.
Reference:
[1] Chinese Chemical Letters, 2011, vol. 22, # 3, p. 253 - 255
[2] Journal of the Chemical Society, 1953, p. 3543,3546
[3] Journal of the Chemical Society, 1947, p. 678,681
2
[ 121-87-9 ]
[ 50358-62-8 ]
Reference:
[1] Journal of the Chemical Society, 1953, p. 3543,3546
[2] Chinese Chemical Letters, 2011, vol. 22, # 3, p. 253 - 255
With sodium t-butanolate; CyJohnPhos;palladium diacetate; In diethylene glycol dimethyl ether; for 2.5h;Reflux;
1. In a 250ml three-mouth flask, <strong>[50358-62-8]8-choro-6-aminoquinoline</strong> (5.0g), 2-choro-N-cyclopropyl-9-(tetrahydro-2H-pyran-2-yl)-9H-purine-6-amine (9.0g), catalyst Pd(OAc)2 (0.25g), ligand 7 (0.25g), sodium tert-butoxide (4.5g) and ethylene glycol dimethyl ether (100ml) are added in turn. The above mixture is stirred and heated to reflux, and the above mixture is reacted under refluxing for 2.5h. The completion of reaction is checked with TCL analysis. The reaction mixture is cooled to room temperature. After filteration, a filter cake is completely washed with ethylene glycol dimethyl ether for 2 times, and a filtrate is concentrated to dry and the reisdue is purified by column chromatography on silica gel to obtain a conjugate (4.6g). The yield is about 37.7% on the basis of aminoquinoline
~ 37.7%
With sodium t-butanolate; CyJohnPhos;palladium diacetate; In 1,2-dimethoxyethane; for 2.5h;Reflux;
In a 250 ml three-mouth flask, <strong>[50358-62-8]8-choro-6-aminoquinoline</strong> (5.0 g), 2-choro-N-cyclopropyl-9-(tetrahydro-2H-pyran-2-yl)-9H-purine-6-amine (9.0 g), catalyst Pd(OAc)2 (0.25 g), ligand 7 (0.25 g), sodium tert-butoxide (4.5 g) and ethylene glycol dimethyl ether (100 ml) are added in turn. The above mixture is stirred and heated to reflux, and the above mixture is reacted under refluxing for 2.5 h. The completion of reaction is checked with TCL analysis. The reaction mixture is cooled to room temperature. After filtration, a filter cake is completely washed with ethylene glycol dimethyl ether for 2 times, and a filtrate is concentrated to dry and the residue is purified by column chromatography on silica gel to obtain a conjugate (4.6 g). The yield is about 37.7% on the basis of aminoquinoline.