Synthesis, biological evaluation, and docking studies of tetrahydrofuran-cyclopentanone-and cyclopentanol-based ligands acting at adrenergic α1- and serotonine 5-HT1A receptors
A series of aralkylphenoxyethylamine and aralkylmethoxyphenylpiperazine compounds was synthesized and their in vitro pharmacological profile at both 5-HT1A receptors and α1-adrenoceptor subtypes was measured by binding assay and func
Convenient synthesis of benzyl and allyl esters using benzyl and allyl 2,2,2-trichloro-acetimidate
Benzyl and allyl 2,2,2-trichloroacetimidate are efficient reagents for the preparation of benzyl and allyl esters of carboxylic acids in the presence of a catalytic amount of boron trifluoride-diethyl ether complex.
Kokotos, George,Chiou, Antonia
p. 168 - 170
(2007/10/03)
Effect of Temperature on Atom Transfer Cyclization Reactions of Allylic α-Iodo Esters and Amides
Atom-transfer cyclizations of allyl iodoacetates and N-allyl-N-methyliodoacetamides are much more efficient at 80 deg C than at 25 deg C.At 80 deg C, β-(iodomethyl) lactones and lactams are formed rapidly and in good yield under standard atom-transfer conditions (sunlamp irradiation of iodide and 10percent hexabutylditin in benzene for 10-60 min).It is proposed that this temperature effect is responsible for some unusual observations by Jolly and Livinghouse in the cyclization of N-cyclohexenyl-N-methyliodoacetamide.The results suggest that the beneficial effect of temperature arises because an increase in the rate of rotation of t he OC-O or OC-N bond in the intermediate radicals begins to convert syn radicals (which cannot cyclize) to anti radicals (which can cyclize).Consistent with this hypothesis, the radical derived from N,N-diallyliodoacetamide (which always has a favorable arrangement for cyclization) closes with excellent efficiency at 25 deg C.
Curran, Dennis P.,Tamine, John
p. 2746 - 2750
(2007/10/02)
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