886367-82-4Relevant academic research and scientific papers
Negishi cross-couplings compatible with unprotected amide functions
Manolikakes, Georg,Dong, Zhibing,Mayr, Herbert,Li, Jinshan,Knochel, Paul
supporting information; experimental part, p. 1324 - 1328 (2009/09/04)
The reaction conditions that allow a general Pd-catalyzed Negishi cross-coupling of a functionalized alkyl, aryl, heteroaryl, and benzylic zinc reagents with aryl acidic hydrogens were investigated. A dry and argon flushed 10 mL Schlenk-tube was charged with N-benzyl-4-bromobenzamide, Pd(OAc) 2, S-PHOS, and THF. 3-pentanoyl-benzylzinc chloride was added slowly over 90 minutes with a syringe pump. The reaction mixture was stirred for 1 hour at 25 °C. The reaction mixture was quenched with a saturated NH 4Cl solution and extracted with diethyl ether. The combined phases were then washed with a aqueous thiourea solution and dried over Na 2SO4. It was observed that the mild conditions considerably increase the ability of the Negishi cross-coupling in the synthesis of complex molecules and natural products.
Oxazolidone derivatives as PR modulators
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, (2008/06/13)
Compounds of the following structure are described: wherein R1, R2, R5, R6, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
