01616nas a2200181   4500008004100000022001400041245014000055210006900195260007200264300000900336490000700345520086300352100001801215700002401233700002201257700002601279856012901305       2007                        eng d  a0305-104800aVersatile method for the preparation of conjugates of peptides with DNA/PNA/analog by employing chemo-selective click reaction in water0 aVersatile method for the preparation of conjugates of peptides w  aGREAT CLARENDON ST, OXFORD OX2 6DP, ENGLANDbOXFORD UNIV PRESScDEC  ae1390 v353 a<p>The specific 1,3 dipolar Hisgen cycloaddition reaction known as `click-reaction' between azide and alkyne groups is employed for the synthesis of peptideoligonucleotide conjugates. The peptide nucleic acids (PNA)/DNA and peptides may be appended either by azide or alkyne groups. The cycloaddition reaction between the azide and alkyne appended substrates allows the synthesis of the desired conjugates in high purity and yields irrespective of the sequence and functional groups on either of the two substrates. The versatile approach could also be employed to generate the conjugates of peptides with thioacetamido nucleic acid (TANA) analog. The click reaction is catalyzed by Cu (I) in either water or in organic medium. In water, similar to 3-fold excess of the peptide-alkyne/azide drives the reaction to completion in 2 h with no side products.</p>1 aGogoi, Khirud1 aMane, Meenakshi, V.1 aKunte, Sunita, S.1 aKumar, Vaijayanti, A.  uhttps://library.ncl.res.in/content/versatile-method-preparation-conjugates-peptides-dnapnaanalog-employing-chemo-selective-001728nas a2200313   4500008004100000022001400041245014500055210006900200260010600269300001200375490000700387520055600394653001500950653002000965653001800985653001601003100002501019700002401044700003101068700002801099700002501127700002101152700002701173700001601200700002301216700002401239700002201263856012901285       2010                        eng d  a0960-894X00aFluconazole analogues containing 2H-1,4-benzothiazin-3(4H)-one or 2H-1,4-benzoxazin-3(4H)-one moieties, a novel class of anti-Candida agents0 aFluconazole analogues containing 2H14benzothiazin34Hone or 2H14b  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcJAN  a722-7250 v203 a<p>As a part of our program to develop new antifungal agents, a series of fluconazole analogues was designed and synthesized wherein one of the triazole moieties in fluconazole was replaced with 2H-1,4-benzothiazin-3(4H)-one or 2H-1,4-benzoxazin-3(4H)-one moiety. The new chemical entities thus synthesized were screened against various fungi and it was observed that the compounds 4a and 4i are potent inhibitors of Candida strains. The structure-activity relationship for these compounds is discussed. (C) 2009 Elsevier Ltd. All rights reserved.</p>10aantifungal10aBenzothiazinone10aBenzoxazinone10aFluconazole1 aBorate, Hanumant, B.1 aMaujan, Suleman, R.1 aSawargave, Sangmeshwer, P.1 aChandavarkar, Mohan, A.1 aVaiude, Sharangi, R.1 aJoshi, Vinay, A.1 aWakharkar, Radhika, D.1 aIyer, Ramki1 aKelkar, Ramesh, G.1 aChavan, Subhash, P.1 aKunte, Sunita, S.  uhttps://library.ncl.res.in/content/fluconazole-analogues-containing-2h-14-benzothiazin-34h-one-or-2h-14-benzoxazin-34h-one-001135nas a2200241   4500008004100000022001400041245010800055210006900163260008600232300001800318490000700336520025300343653001900596653001600615653001800631653001300649653001200662100002700674700002200701700002400723700002300747856012300770       2011                        eng d  a0039-791100aExploration of L-proline-catalyzed -aminoxylation of aldehyde to (S)-guaifenesin-related drug molecules0 aExploration of Lprolinecatalyzed aminoxylation of aldehyde to Sg  a325 CHESTNUT ST, SUITE 800, PHILADELPHIA, PA 19106 USAbTAYLOR & FRANCIS INCcMAY  aPII 9371379300 v413 a<p>[image omitted] An efficient enantioselective synthesis of (S)-guaifenesin with 99% ee using L-proline-catalyzed -aminoxylation of aldehyde as key step is described and explored for asymmetric syntheses of (S)-moprolol and (R)-methocarbamol.</p>10a-Aminoxylation10aguaifenesin10amethocarbamol10amoprolol10aProline1 aPanchgalle, Sharad, P.1 aKunte, Sunita, S.1 aChavan, Subhash, P.1 aKalkote, Uttam, R.  uhttps://library.ncl.res.in/content/exploration-l-proline-catalyzed-aminoxylation-aldehyde-s-guaifenesin-related-drug-001447nas a2200253   4500008004100000022001400041245015200055210006900207260010300276300001200379490000700391520042600398653003100824653004400855653001700899653002200916653001400938653003000952653001400982100002600996700002201022700001901044856013001063       2011                        eng d  a0376-469900aRegioselective NaBH4 and DIBAL-H reductions of 3,4-dimethoxyhomopiperonylphthalimide: concise and efficient synthesis of nuevamine and isonuevamine0 aRegioselective NaBH4 and DIBALH reductions of 34dimethoxyhomopip  aANUSANDHAN BHAWAN, 2 RAFI MARG, NEW DELHI, 110001, INDIAbCOUNCIL SCIENTIFIC & INDUSTRIAL REScJUN  a868-8710 v503 a<p>Facile synthesis of nuevamine and isonuevamine has been reported via the regioselectivc reduction of hindered and unhindered carbonyl groups of 3,4-dimethoxyhomopiperonylphthalimide, respectively using sodium borohydridc and diisobutylaluminum hydride, Mowed by an acid catalyzed intramolecular dehydrative cyclization pathways. The chemistry involved in obtaining the regioselectivity has been discussed in brief.</p>10a6-dimethoxyhomophthalimide10aintramolecular dehydrative cyclizations10aisonuevamine10aN-Homopiperonyl-510anuevamine10aregioselective reductions10asynthesis1 aWakchaure, Prasad, B.1 aKunte, Sunita, S.1 aArgade, N., P.  uhttps://library.ncl.res.in/content/regioselective-nabh4-and-dibal-h-reductions-34-dimethoxyhomopiperonylphthalimide-concise-001096nas a2200193   4500008004100000022001400041245010900055210006900164260007100233300001400304490000700318520032700325100003300652700002300685700002200708700002400730700002200754856012600776       2013                        eng d  a1523-706000aAsymmetric N-heterocyclic carbene (NHC)-catalyzed annulation of modified enals with enolizable aldehydes0 aAsymmetric Nheterocyclic carbene NHCcatalyzed annulation of modi  a1155 16TH ST, NW, WASHINGTON, DC 20036 USAbAMER CHEMICAL SOCcOCT  a5202-52050 v153 a<p>N-Heterocyclic carbene (NHC)-catalyzed highly enantioselective lactonization of modified enals with enolizable aldehydes, proceeding via the alpha,beta-unsaturated acylazolium intermediates, is reported. The reaction results in the asymmetric synthesis of synthetically important 4,5-disubstituted dihydropyranones.</p>1 aYetra, Santhivardhana, Reddy1 aKaicharla, Trinadh1 aKunte, Sunita, S.1 aGonnade, Rajesh, G.1 aBiju, Akkattu, T.  uhttps://library.ncl.res.in/content/asymmetric-n-heterocyclic-carbene-nhc-catalyzed-annulation-modified-enals-enolizable-001566nas a2200169   4500008004100000022001400041245012800055210006900183260010600252300001400358490000700372520081800379100002201197700002201219700002601241856012901267       2014                        eng d  a0957-416600aNew organocatalyst derived from abietic acid and 4-hydroxy-L-proline for direct asymmetric aldol reactions in aqueous media0 aNew organocatalyst derived from abietic acid and 4hydroxyLprolin  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcOCT  a1292-12970 v253 a<p>Enantioselective direct aldol reactions were carried out in aqueous media with a new organocatalyst that was derived from 4-hydroxy-L-proline and abietic acid via a simple and convenient synthetic protocol with a high overall yield (75%). The new organocatalyst was used for aldol reactions between substituted aromatic aldehydes and various ketones in the presence of several acid additives in aqueous media. The corresponding aldol products were obtained in high isolated yields (up to 99%) and with high anti-diastereoselectivities (up to 94%) and enantioselectivities (&gt;99.9%). The catalyst loading can be efficiently reduced to only 1 mol %. The aldol reactions were found to be extremely fast which is very unusual in organocatalyzed reactions in water. (C) 2014 Elsevier Ltd. All rights reserved.</p>1 aBhowmick, Sudipto1 aKunte, Sunita, S.1 aBhowmick, Kartick, C.  uhttps://library.ncl.res.in/content/new-organocatalyst-derived-abietic-acid-and-4-hydroxy-l-proline-direct-asymmetric-aldol-001302nas a2200205   4500008004100000022001400041245013700055210006900192260011000261300001600371490000700387520043100394100002300825700003300848700001700881700002200898700002400920700002200944856013000966       2014                        eng d  a1359-734500aN-Heterocyclic carbene-catalyzed enantioselective synthesis of functionalized cyclopentenes via alpha,beta-unsaturated acyl azoliums0 aNHeterocyclic carbenecatalyzed enantioselective synthesis of fun  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcOCT  a14539-145420 v503 a<p>Highly enantioselective NHC-organocatalyzed synthesis of functionalized cyclopentenes proceeding via alpha,beta-unsaturated acyl azolium intermediates is reported. The organocascade reaction of modified enals with malonic ester derivatives having a gamma-benzoyl group involves the Michael-intramolecular aldol-beta-lactonization-decarboxylation sequence to deliver cyclopentenes in good yields and excellent ee values.</p>1 aMondal, Santigopal1 aYetra, Santhivardhana, Reddy1 aPatra, Atanu1 aKunte, Sunita, S.1 aGonnade, Rajesh, G.1 aBiju, Akkattu, T.  uhttps://library.ncl.res.in/content/n-heterocyclic-carbene-catalyzed-enantioselective-synthesis-functionalized-cyclopentenes-001320nas a2200169   4500008004100000022001400041245010800055210006900163260011000232300001600342490000600358520058800364100002200952700002200974700002600996856012801022       2014                        eng d  a2046-206900aSmallest organocatalyst in highly enantioselective direct aldol reaction in wet solvent-free conditions0 aSmallest organocatalyst in highly enantioselective direct aldol   aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcMAY  a24311-243150 v43 a<p>The catalytic efficacy of the smallest organocatalyst, L-proline hydrazide, prepared from a cheaply available natural amino acid, such as L-proline, was studied for the direct asymmetric aldol reaction of various ketones with aromatic aldehydes at room temperature in the presence of several acid additives. A loading of 10 mol% of catalyst 1 and p-toluenesulphonic acid as an additive was employed in this reaction, and good yields (up to 99%) with high anti/syn diastereoselectivities (up to 95 : 5) and enantioselectivities (up to &gt;99.9%) were achieved in aqueous media.</p>1 aBhowmick, Sudipto1 aKunte, Sunita, S.1 aBhowmick, Kartick, C.  uhttps://library.ncl.res.in/content/smallest-organocatalyst-highly-enantioselective-direct-aldol-reaction-wet-solvent-free-001672nas a2200229   4500008004100000022001400041245016200055210006900217260010300286300001000389490000700399520073200406653001901138653001801157653002501175653002601200653002001226100002201246700002201268700002601290856012601316       2015                        eng d  a0376-469900aComprehensive study on the effect of acid additives in 1(R),2(R)-Bis[(S)-prolinamido]cyclohexane catalyzed direct asymmetric aldol reactions in aqueous media0 aComprehensive study on the effect of acid additives in 1R2RBisSp  aANUSANDHAN BHAWAN, 2 RAFI MARG, NEW DELHI, 110001, INDIAbCOUNCIL SCIENTIFIC & INDUSTRIAL REScJAN  a84-920 v543 a<p>The catalytic efficacy of (1R,2R)-bis[(S)-prolinamido]cyclohexane 1, prepared from the readily available natural amino acid L-proline has been studied for the direct asymmetric aldol reaction of cyclohexanone with substituted benzaldehydes at room temperature in presence of various acid additives. A wide variety of acids e.g. aliphatic fatty acid, chiral acid, sulphonic acid, aromatic acid, etc. have been used as additive for the aldol reaction in aqueous media. A loading of 10 mol% of catalyst 1 is employed in this reaction, and good yields (up to 98% yield), diastereoselectivity (up to 96% de) and enantioselectivities (up to 87% ee) can be achieved in aqueous media within very short reaction time (1-4 hours).</p>10aacid additives10aaqueous media10aAsymmetric synthesis10adirect aldol reaction10aorganocatalysis1 aBhowmick, Sudipto1 aKunte, Sunita, S.1 aBhowmick, Kartick, C.  uhttps://library.ncl.res.in/content/comprehensive-study-effect-acid-additives-1r2r-biss-prolinamidocyclohexane-catalyzed-0