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• W2897056676 abstract "Tetrahydrophthalazine derivatives have found important applications in pharmaceutical research, but existing synthetic methods are unable to access them regio- and stereoselectively. Here, a new approach is presented that addresses these challenges by utilizing a 6-endo-trig radical cyclization in the key step. The desired tetrahydrophthalazines can be accessed in high yields (55-98 %) and high diastereoselectivities for the trans-product (>95:5) starting either from readily accessible hydrazones, or from the corresponding aldehydes and substituted Boc-hydrazides in a one-pot process. The synthetic versatility of the tetrahydrophthalazine core was demonstrated by its straightforward conversion to dihydro-phthalazines, phthalazines, or pyrazolo dione derivatives. Furthermore, the N-N bond was reduced to afford a new route to 1,4-diamines." @default.
• W2897056676 created "2018-10-26" @default.
• W2897056676 creator A5014298922 @default.
• W2897056676 creator A5036921910 @default.
• W2897056676 creator A5070204678 @default.
• W2897056676 creator A5075814512 @default.
• W2897056676 creator A5083279299 @default.
• W2897056676 date "2018-12-12" @default.
• W2897056676 modified "2023-09-24" @default.
• W2897056676 title "Regiocontrolled and Stereoselective Syntheses of Tetrahydrophthalazine Derivatives using Radical Cyclizations" @default.
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