Regorafenib synthesis
- Product Name:Regorafenib
- CAS Number:755037-03-7
- Molecular formula:C21H15ClF4N4O3
- Molecular Weight:482.82
Du, Fangyu; Zhou, Qifan; Shi, Yajie; Yu, Miao; Sun, Wenjiao; Chen, Guoliang. A new pathway via intermediate 4-amino-3-fluorophenol for the synthesis of regorafenib. Synthetic Communications. Volume 49. Issue 4. Pages 576-586. Journal; Online Computer File. (2019).
757251-39-1
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$11.00/250mg
42558-54-3
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$10.00/5g
320-51-4
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$6.00/10g
755037-03-7
451 suppliers
$25.00/5 mg
Yield:755037-03-7 96.8%
Reaction Conditions:
with dmap in N,N-dimethyl-formamide at 140; for 4 h;Green chemistry;Temperature;
Steps:
8 Preparation of regomafenib (I)
To the reaction flask, a compound IV 13.27 g, a compound V 9.93 g, a methyl isobutyryl acetate 7.32 g, a 4-dimethylaminopyridine 6.21 g, and 800 ml of DMF were sequentially added, and the mixture was stirred and dissolved, and the temperature was controlled at 140 ° C for 4 h. The TLC monitors the completion of the reaction. The reaction was stopped, the temperature was lowered to room temperature, and ethyl acetate was added for extraction. The organic layer was separated and concentrated under reduced pressure to give 25.55 g, product yield 96.8%, purity 99.93%.
References:
Shandong Luoxin Pharmaceutical Group Hengxin Pharmaceutical Co., Ltd.;Liu Zhenteng;Hou Junkai;Fan Xuezhen;Yang Taotao CN108329260, 2018, A Location in patent:Paragraph 0014; 0037; 0040; 0043-0046
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327-78-6
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755037-03-7
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$25.00/5 mg
757251-39-1
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$11.00/250mg
868-84-8
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320-51-4
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$6.00/10g
755037-03-7
451 suppliers
$25.00/5 mg
757251-39-1
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$11.00/250mg
1737-36-6
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$15.00/1g
755037-03-7
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$25.00/5 mg
96-49-1
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757251-39-1
234 suppliers
$11.00/250mg
320-51-4
457 suppliers
$6.00/10g
755037-03-7
451 suppliers
$25.00/5 mg