IR@IIIM - Indian Institute of Integrative Medicine (CSIR)
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Kinetic resolution of 1-chloro-3-(1-naphthyloxy)-2-propanol, an intermediate in the synthesis of beta-adrenergic receptor blockers.
(R)- and (S)-1-chloro-3-(1-naphthyloxy)-2-propanol are intermediates in the synthesis of beta-adrenergic blocking agents and antihypertensive drugs such as propranolol and nadoxolol. Herein, improvement in the preparation of racemic 1-chloro-3-(1-naphthyloxy)-2-propanol generated from 1-naphthol and epichlorohydrin are reported. In addition, kinetic resolution studies have been conducted to obtain both (R) and (S)-1-chloro-3-(1-naphthyloxy)-2-propanol. These compounds were obtained in highly optically pure form by the stereoselective hydrolysis of its acyl derivatives using whole cell preparations containing enzymes from native sources. The results were compared with those obtained using commercial lipases
New chemo and chemo-enzymatic synthesis of β-benzyl-γ-butyrolactones
b-Benzyl-g-butyrolactones, important intermediates for the synthesis of butyrolactone lignands, have been synthesized by a new route involving preparation of a-b-unsaturated formyl esters. The formyl esters can easily be converted into the desired butyrolactones either through chemical transformations or by enzymatic methods
Unequivocal total assignment of13C and1H NMR spectra of some pyrido[1,2-a]pyrimidine derivatives by 2D-NMR
We report the total assignments of the 13C and 1H NMR spectra of some 4-methyl-2-oxo-(2H)-pyrido[1,2-a]pyrimidine and 2-methyl-4-oxo-(4H)-pyrido[1,2-a]pyrimidine derivatives. The products were characterized by
1H and 13C NMR and reported data for similar compounds.
No comparative data for the two sets of isomeric
compounds with respect to 13C and 1H NMR have been
reported to date. We made some detailed studies of the
2D NMR spectra of these compounds and observed that
assignments made for non-protonated carbon atoms by
us and those reported in the literature for similar compounds need correction. The revised assignments were
made on the basis of heteronuclear single quantum
correlation (HSQC) and heteronuclear multiple bond
correlation (HMBC) techniques. Copyright 2003 John
Wiley & Sons, Ltd
Variation of oil content in a new clone of Jamrosa ‘RL‐931’(Cymbopogon nardusvar. confertiflorus× C. jwarancusa)during one year of crop growth
The effect of seasonal changes on oil content of a new clone of Jamrosa 'RL-931'(Cymbopogon nardus var. confertiflorus × C.jwarancusa) was investigated during 1998-99. The pre-monsoon and onset of the monsoon period
(May-July) was characterised by a higher oil content, whereas the post-monsoon and winter period (August-December) showed a comparatively lower oil content. The quality of the oil is best in May-July. High temperature and low humidity favours the accumulation of geraniol, geranyl acetate, and a low citral content in the oil. Maximum oil content was recorded when both maximum and
minimum temperatures were high
Reaction of Resorcinol with Mesityl Oxide: Synthesis of 2,2-Dimethyl-4-formyl- 7-methoxy-(2H)-1-benzopyran
Synthesis of 2,2-dimethyl-4-formyl-7-methoxy-(2H)-1-benzopyran has been achieved by a three step reaction sequence, wherein the key step has been the preparation of 7-hydroxy-2,2,4-trimethyl-(2H)-1-benzopyran by a novel condensation reaction between resorcinol and mesityl oxide in presence of polyphosphoric acid (PPA)
AN UNEQUIVOCAL SYNTHESIS OF 4-METHYL-2-OXO-(2H)-PYRIDO- [1,2-a]PYRIMIDINES1*
An unequivocal high yielding synthesis of 4-methyl-2-oxo-
(2H)-pyrido[1,2-a]pyrimidines from N-(1,3-dioxobutyl)-2-
amino pyridines/picolines/quinoline, is being reported
Hepatoprotective activity of indigtone-a bioactive fraction fromIndigofera tinctoria Linn.
A bioactive fraction, indigtone (FA), obtained by fractionation of a petroleum ether extract of the aerial
parts of Indigofera tinctoria, showed significant dose related hepatoprotective activity against CCl4
induced liver injury in rats and mice. Hexobarbitone induced ‘sleeptime’, zoxazolamine induced ‘paralysis
time’, levels of transaminases, bilirubin and total protein in serum were employed as indices of liver
injury. Pre and post treatment with FA significantly reversed the majority of the parameters altered by
the hepatotoxin. This indicated the preventive and restorative effect of FA in the process of CCl4 induced
liver damage. The fraction possessed a high therapeutic ratio, as no mortality was observed up to a dose
of 2g/kg p.o. in mic
A New Glycoside, 3-o-Demethylcolchicine-3-o-α-d-Glucopyranoside, fromGloriosa SuperbaSeeds
A new colchicine glycoside, 3-O-demethylcolchicine-3-O-a-~-glucopyranosidhea,s been isolated from Gloriosa superba seeds. The assigned structure has been corroborated by spectroscopic data and enzymatic hydrolysis
Adaptogenic activity of a novel, withanolide-free aqueous fraction from the roots ofWithania somnifera Dun.
The practitioners of the traditional Indian system of medicine regard Withania somnifera Dun. as the ‘Indian ginseng’. A new withanolide-free aqueous fraction was isolated from the roots of this plant and was evaluated for putative antistress activity against a battery of tests such as hypoxia time, antifatigue effect, swimming performance time, swimming induced gastric ulceration and hypothermia, immobilization induced gastric ulceration, autoanalgesia and biochemical changes in the adrenal glands. This bioactive fraction exhibited significant antistress activity in a dose-related manner in all the parameters studied. The extract of Withania somnifera root (a commercial preparation available locally) was used to
compare the results. A preliminary acute toxicity study in mice showed a good margin of safety. Copyright
� 2001 John Wiley & Sons, Ltd
Microwave Induced Acetoacetylation of Hetaryl and Aryl Amines
Acetoacetylation of hetaryl and aryl amines by interaction with ethyl acetoacetate under microwave irradiation, without any catalyst and/or solvent, is reported