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Rational design and synthesis of new PARP1 inhibitors

✍ Scribed by Leonid V. Romashov; Alexey A. Zeifman; Alexandra L. Zakharenko; Fedor N. Novikov; Viktor S. Stroilov; Oleg V. Stroganov; Germes G. Chilov; Svetlana N. Khodyreva; Olga I. Lavrik; Ilya Yu. Titov; Igor V. Svitan’ko

Book ID
113798718
Publisher
Royal Society of Chemistry
Year
2012
Tongue
English
Weight
344 KB
Volume
22
Category
Article
ISSN
0959-9436

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Scheme 1. Synthesis of IFG (1) and IFG derivatives 2-8. a) CH 2 = C(OMe)Me, TsOH•H 2 O, THF, 1.5 h, 0 8C (53 %); b) Tf 2 O, pyridine, CH 2 Cl 2 , 2 h, À78!0 8C; then KCN, 18[crown]-6, DMF, 16 h, RT (80 %); c) RMgX, Et 2 O, 2 h, RT; then NaBH 4 , overnight, RT (65-74 %); d) H 2 , 20 % Pd(OH) 2 /C, Ac