01285nas a2200241   4500008004100000022001400041245010300055210006900158260000900227300001400236490000700250520045100257653001600708653002400724653002100748653001600769653004100785100002400826700002300850700001600873700002200889856013200911       2015                        eng d  a0040-402000aChirality induction and chiron approaches to enantioselective total synthesis of alpha-lipoic acid0 aChirality induction and chiron approaches to enantioselective to  cJUN   a4213-42180 v713 a<p>An efficient, short and convenient asymmetric synthesis of (R)-(+)-lipoic acid in seven steps from chiral hydroxy aldehyde with 32.5% overall yield is described. Synthesis of S and R enantiomers of a-lipoic acid from cis-1,4-butene diol derived chiral lactone is reported with 34 % overall yield. The present synthesis involves use of simple reaction conditions making it a convenient synthesis. (C) 2015 Elsevier Ltd. All rights reserved.</p>10aChiral pool10aChirality induction10aenantioselective10aLipoic acid10asharpless asymmetric dihydroxylation1 aChavan, Subhash, P.1 aPawar, Kailash, P.1 aPraveen, Ch1 aPatil, Niteen, B.  uhttps://library.ncl.res.in/content/chirality-induction-and-chiron-approaches-enantioselective-total-synthesis-alpha-lipoic-acid01295nas a2200193   4500008004100000022001400041245012000055210006900175260010600244300001200350490000700362520048500369100002500854700002300879700002200902700002300924700002400947856013000971       2015                        eng d  a0957-416600aTotal synthesis of (R)-lipoic acid and (S)-lipoic acid via an Mn (III)-salen-catalyzed oxidative kinetic resolution0 aTotal synthesis of Rlipoic acid and Slipoic acid via an Mn IIIsa  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcMAR  a281-2870 v263 a<p>The asymmetric synthesis of both the antipodes of alpha-lipoic acid is described. The total synthesis of racemic and asymmetric lipoic acid is achieved from propane 1,3-diol. This work reports the use of Mn (III)-salen-catalyzed oxidative kinetic resolution as the key step to obtain enantiomerically pure (R)- and (S)-lipoic acid. The undesired product formed during the resolution can be recycled to achieve the desired isomer. (C) 2015 Elsevier Ltd. All rights reserved.</p>1 aPurude, Abhijeet, N.1 aPawar, Kailash, P.1 aPatil, Niteen, B.1 aKalkote, Uttam, R.1 aChavan, Subhash, P.  uhttps://library.ncl.res.in/content/total-synthesis-r-lipoic-acid-and-s-lipoic-acid-mn-iii-salen-catalyzed-oxidative-kinetic-001431nas a2200253   4500008004100000022001400041245013700055210006900192260000800261300001400269490000700283520055100290653002200841653001500863653001600878653001200894653002300906100002400929700002200953700002200975700002500997700002801022856012701050       2020                        eng d  a0039-788100aScalable synthesis of 3-Ethyl-4-methyl-1,5-dihydro-2H-pyrrol-2-one: an important building block of the antidiabetic drug glimepiride0 aScalable synthesis of 3Ethyl4methyl15dihydro2Hpyrrol2one an impo  cNOV  a3480-34840 v523 a<p>A four-step, practical, and easily scalable synthesis of 3-ethyl-4-methyl-1,5-dihydro-2H-pyrrol-2-one, an important building block of the antidiabetic drug glimepiride, has been accomplished. Key features are the synthesis of 3-methyl-4-hydroxy-2-butenolide in water and triflic acid mediated N-benzyl lactam N-deprotection. The main advantages of this process are the scalable synthetic route and decreased number of reaction steps, which paves the way for the industrial-scale synthesis of 3-ethyl-4-methyl-1,5-dihydro-2H-pyrrol-2-one.</p>
10aantidiabetic drug10aButenolide10aglimepiride10alactams10ascalable synthesis1 aChavan, Subhash, P.1 aPawar, Ambaji, A.1 aPatil, Niteen, B.1 aKadam, Appasaheb, L.1 aShinde, Shrikrishna, S.  uhttps://library.ncl.res.in/content/scalable-synthesis-3-ethyl-4-methyl-15-dihydro-2h-pyrrol-2-one-important-building-block01085nas a2200241   4500008004100000022001400041245016100055210006900216260000900285300001100294490000700305520021100312653001600523653002400539653002000563653001900583653001700602100002400619700002300643700002200666700002400688856013100712       2021                        eng d  a0040-403900aApplication of allylic amine formation from aziridine-2-ol under appel reaction condition: synthesis of N-(tert-butoxycarbonyl)-D-vinyl glycine methyl ester0 aApplication of allylic amine formation from aziridine2ol under a  cJUN   a1531190 v733 a<p>PPh3/I-2/imidazolde mediated allyl amine formation from aziridine-2-alcohol was explored for the synthesis of N-(tert-butoxycarbonyl)-D-vinyl glycine methyl ester. (C) 2021 Published by Elsevier Ltd.</p>10aAllyl amine10aAziridine-2-alcohol10aAziridinium ion10aBirch reaction10aRing opening1 aChavan, Subhash, P.1 aKawale, Sanket, A.1 aPatil, Niteen, B.1 aKalbhor, Dinesh, B.  uhttps://library.ncl.res.in/content/application-allylic-amine-formation-aziridine-2-ol-under-appel-reaction-condition-synthesis01605nas a2200241   4500008004100000022001400041245010400055210006900159260000900228300001600237490000700253520076200260653002001022653003201042653001601074653002401090653002701114100002201141700002601163700002401189700002301213856012701236       2021                        eng d  a0947-653900aMulti-step synthesis of miltefosine: integration of flow chemistry with continuous mechanochemistry0 aMultistep synthesis of miltefosine integration of flow chemistry  cDEC   a17695-176990 v273 aHerein we report for the first time, an advanced continuous flow synthesis of the blockbuster Leishmaniasis drug miltefosine from simple starting materials by a sequence involving four steps of chemical transformation including a continuous mechanochemical step. First three reaction steps were performed in simple tubular reactors in a telescopic mode, while in the last step the product precipitated from the 3(rd) step was used for a continuous mechanochemical synthesis of miltefosine. When compared to a typical batch protocol that takes 15 h, miltefosine was obtained in 58 % overall yield in flow synthesis mode at the laboratory scale in a total residence time 34 min at synthesis rate of 10 g/hr, which is sufficient to treat 4800 patients per day.10acontinuous flow10acontinuous mechanochemistry10amiltefosine10amultistep synthesis10areactive intermediates1 aPatil, Niteen, B.1 aAtapalkar, Ranjit, S.1 aChavan, Subhash, P.1 aKulkarni, Amol, A.  uhttps://library.ncl.res.in/content/multi-step-synthesis-miltefosine-integration-flow-chemistry-continuous-mechanochemistry