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Judicious application of allyl protecting groups for the synthesis of 2-morpholin-4-yl-4-oxo-4H-chromen-8-yl triflate, a key precursor of DNA-dependent protein kinase inhibitors.
Organic Letters ( IF 4.9 ) Pub Date : 2006 Dec 21 , DOI: 10.1021/ol062297x Sonsoles Rodriguez Aristegui 1 , Marine Desage El-Murr 1 , Bernard T. Golding 1 , Roger J. Griffin 1 , Ian R. Hardcastle 1
Organic Letters ( IF 4.9 ) Pub Date : 2006 Dec 21 , DOI: 10.1021/ol062297x Sonsoles Rodriguez Aristegui 1 , Marine Desage El-Murr 1 , Bernard T. Golding 1 , Roger J. Griffin 1 , Ian R. Hardcastle 1
Affiliation
[Structure: see text] 2-morpholin-4-yl-4-oxo-4H-chromen-8-yl 2,2,2-trifluoromethanesulfonate is a key intermediate for the synthesis of the DNA-dependent protein kinase (DNA-PK) inhibitor 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one (NU7441). Two improved methods for the synthesis of this triflate have been developed: (A) in 35% overall yield, through modification of the published route, and (B) in 15% overall yield, by a new route employing a Baker-Venkataraman rearrangement to enable generation of the chromenone scaffold. Both syntheses depend on the judicious use of allyl protecting groups.
中文翻译：
烯丙基保护基团在2-吗啉-4-基-4-氧-4-氧-4H-铬基-8-三氟甲磺酸酯（DNA依赖性蛋白激酶抑制剂的关键前体）的合成中的明智应用。
[结构：见正文] 2-吗啉-4-基-4-氧代-4H-铬n-8-基2,2,2-三氟甲磺酸盐是合成DNA依赖性蛋白激酶（DNA-PK）的关键中间体）抑制剂8-二苯并噻吩-4-基-2-吗啉-4-基-铬基-4-酮（NU7441）。已开发出两种改进的合成三氟甲磺酸酯的方法：（A）通过修饰已公开的路线使总收率达到35％，（B）通过采用Baker-Venkataraman重排反应的新路线来提高总收率15％。能够生成色酮支架。两种合成都取决于对烯丙基保护基的明智使用。
更新日期：2017-01-31
中文翻译：
烯丙基保护基团在2-吗啉-4-基-4-氧-4-氧-4H-铬基-8-三氟甲磺酸酯（DNA依赖性蛋白激酶抑制剂的关键前体）的合成中的明智应用。
[结构：见正文] 2-吗啉-4-基-4-氧代-4H-铬n-8-基2,2,2-三氟甲磺酸盐是合成DNA依赖性蛋白激酶（DNA-PK）的关键中间体）抑制剂8-二苯并噻吩-4-基-2-吗啉-4-基-铬基-4-酮（NU7441）。已开发出两种改进的合成三氟甲磺酸酯的方法：（A）通过修饰已公开的路线使总收率达到35％，（B）通过采用Baker-Venkataraman重排反应的新路线来提高总收率15％。能够生成色酮支架。两种合成都取决于对烯丙基保护基的明智使用。
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