128145-39-1Relevant academic research and scientific papers
Eco-friendly reactions in PEG-400: A highly efficient and green approach for stereoselective access to multisubstituted 3,4-dihydro-2(1: H)-quinazolines using 2-aminobenzylamines
Sharma, Nutan,Sharma, Pankaj,Bhagat, Sunita
, p. 8721 - 8731 (2018/03/08)
An efficient and stereoselective synthesis of novel 3,4-dihydro-2(1H)-quinazolines has been developed through cyclization reactions of 2-aminobenzylamines with α-oxoketene dithioacetals using PEG-400 as an inexpensive, easy to handle, non-toxic and recycl
Stable and Rapid Thiol Bioconjugation by Light-Triggered Thiomaleimide Ring Hydrolysis
Kalia, Dimpy,Pawar, Sharad P.,Thopate, Jyoti S.
, p. 1885 - 1889 (2017/02/05)
Maleimide-mediated thiol-specific derivatization of biomolecules is one of the most efficacious bioconjugation approaches currently available. Alarmingly, however, recent work demonstrates that the resulting thiomaleimide conjugates are susceptible to breakdown via thiol exchange reactions. Herein, we report a new class of maleimides, namely o-CH2NHiPr phenyl maleimides, that undergo unprecedentedly rapid ring hydrolysis after thiol conjugation to form stable thiol exchange-resistant conjugates. Furthermore, we overcome the problem of low shelf lives of maleimide reagents owing to their propensity to undergo ring hydrolysis prior to bioconjugation by developing a photocaged version of this scaffold that resists ring hydrolysis. UV irradiation of thiol bioconjugates formed with this photocaged maleimide unleashes rapid thiomaleimide ring hydrolysis to yield the desired stable conjugates within 1 h under gentle, ice-cold conditions.
Benzothiadiazinyl-indole derivatives and their use as serotonin receptor ligands
-
, (2008/06/13)
Compounds having the formula: in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3, R1and R2are each hydrogen or C1-4alkyl, R3, R4and R5are each hydrogen, C1-4alkyl, optionally substituted phenyl or optionally substituted phenyl-C1-4alkyl, or R3and R4together form an alkylene link of formula -(CH2)3- or -(CH2)4-, or R4and R5together with the carbon atom to which they are attached form a C3-6cycloalkyl group, R6is C1-4alkyl, C1-4alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino, the dotted line represents an optional double bond, and the fluorine atom is attached at the 6 or 7-position; and salts and esters thereof, are binding to the 5-HT serotonin receptor and are useful in the treatment of CNS disorders.
1H-2,1,3-benzothiadiazine-2,2-dioxide compounds or derivatives thereof
-
, (2008/06/13)
A pharmaceutical compound having the formula: STR1 in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3, R1 and R2 are each hydrogen or C1-4 alkyl, R3, R4 and R5 are each hydrogen, C1-4 alkyl, optionally substituted phenyl or optionally substituted phenyl-C1-4 alkyl, or R3 and R4 together form an alkylene link of formula --(CH2)3 -- or --(CH2)4 --, or R4 and R5 together with the carbon atom to which they are attached form a C3-6 cycloalkyl group, R6 is C1-4 alkyl, C1-4 alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino, the dotted line represents an optional double bond, and the fluorine atom is attached at the 6 or 7-position; and salts and esters thereof.
HEXAHYDRO-1,3,2-DIAZAPHOSPHORINES. IX. SYNTHESIS AND CHEMICAL REACTIONS OF 1- AND 3-MONOALKYL(ARYL)-1,2,3,4-TETRAHYDRO-1,3,2-BENZODIAZAPHOSPHORINES
Nifant'ev, E. E.,Zavalishina, A. I.,Dorogotovtsev, S. S.,Orzhekovskaya, E. I.,Nurkulov, N. N.,et al.
, p. 1642 - 1651 (2007/10/02)
Previously unknown 1- and 3-monoalkyl(aryl)-1,2,3,4-tetrahydro-1,3,2-benzodiazaphosphor(III)ines were synthesized, and some chemical reactions resulting in an increase in the coordination number of the phosphorus atom were studied.The structure of the compounds obtained was proved by 1H, 13C, and 31P NMR spectroscopy.
