@article {43222, title = {Mild and efficient method for the synthesis of vinylogous carbamates from alkyl azides}, journal = {Tetrahedron Letters}, volume = {46}, year = {2005}, month = {FEB}, pages = {979-982}, abstract = {A mild and efficient one-pot method for the synthesis of vinylogous carbamates is reported starting from alkyl azides under a hydrogen atmosphere using 10\% Pd/C. The resulting products are useful intermediates for the synthesis of heterocyclic compounds, natural products, and in peptidomimetics. (C) 2004 Elsevier Ltd. All rights reserved.}, doi = {10.1016/j.tetlet.2004.12.047}, author = {Reddy, D. Srinivasa and Rajale, T. V. and Shivakumar, K. and Iqbal, Javed} } @article { ISI:000379577800033, title = {Molecules with O-acetyl group protect protein glycation by acetylating lysine residues}, journal = {RSC Advances}, volume = {6}, number = {70}, year = {2016}, month = {JUL}, pages = {65572-65578}, publisher = {ROYAL SOC CHEMISTRY}, address = {THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND}, abstract = {

Pharmaceutical intervention for reduction of advanced glycation end products (AGEs) is considered as a therapeutic strategy to attenuate the pathogenesis of diabetes. Many molecules have been reported to possess antiglycation activity, one such example is acetylsalicylic acid (aspirin). It protects proteins from glycation by acetylating the lysine residues. Therefore, in this study we have synthesized and screened molecules containing free N-acetyl, O-acetyl and acetophenone groups. All the selected molecules in this study showed glycation inhibition but interestingly, only molecules with O-acetyl but not N-acetyl and acetophenone groups were capable of acetylating lysine residue. Furthermore, we have demonstrated that pre-acetylation or aspirin treatment prior to the induction of diabetes helps in reducing HbA1c and AGE formation in the streptozotocin induced diabetic mice. Hence pre-acetylation may have an additional therapeutic efficacy of reducing AGE levels in vivo. Incorporation of O-acetyl group into anti-diabetic molecules could be a useful strategy, as it may have an additive effect in reducing AGEs. Identification of such novel acetylating agents represents a new area in the drug discovery process.

}, issn = {2046-2069}, doi = {10.1039/c6ra11313c}, author = {Vannuruswamy, Garikapati and Jagadeeshaprasad, Mashanipalya G. and Kashinath, K. and Kesavan, Suresh K. and Bhat, Shweta and Korwar, Arvind M. and Chougale, Ashok D. and Boppana, Ramanamurthy and Reddy, D. Srinivasa and Kulkarni, Mahesh J.} } @article { ISI:000380599800018, title = {Multi-gram scale synthesis of hunanamycin A, an antibiotic natural product from the marine source}, journal = {Tetrahedron Letters}, volume = {57}, number = {32}, year = {2016}, month = {AUG}, pages = {3662-3663}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

A simple, practical, and biomimetic approach to access antibiotic natural product hunanamycin A starting from readily available inexpensive material Riboflavin is disclosed here. The present synthesis consists of three operationally simple, protecting group free steps and it is far superior when compared with the previous route. Using this route one can make multi-gram quantities of the natural product which will help in further biological assays, in particular exploring the potential of treating food infections. (C) 2016 Elsevier Ltd. All rights reserved.

}, keywords = {Antibacterial, Biomimetic synthesis, Gram scale synthesis, Natural product, Riboflavin}, issn = {0040-4039}, doi = {10.1016/j.tetlet.2016.07.003}, author = {Shingare, Rahul D. and Farhana, Sa Ada and Reddy, D. Srinivasa} } @article {44648, title = {Multi-step continuous flow synthesis of the cystic fibrosis medicine ivacaftor}, journal = {Reaction Chemistry \& Engineering}, volume = {3}, year = {2018}, month = {AUG}, pages = {520-526}, abstract = {

A continuous flow ozonolysis method combined with a multi-step flow sequence is developed for the synthesis of the drug ivacaftor for the first time. Safe ozonolysis, a continuous flow quadruple reaction to construct a quinolone scaffold, and inline extraction followed by continuous phase separation are the key features of the present work. The feasibility of using a continuous mixed flow reactor, commonly referred to as a continuous stirred tank reactor (CSTR), is also investigated for the relatively slow reaction step. The current integrated multi-step flow synthesis can produce 7.2 g of the drug ivacaftor per day on a laboratory scale, which is sufficient to treat 50 patients per day. The present route can also be used as a general route for the synthesis of other related drugs such as quinolone antibiotics.

}, issn = {2058-9883}, doi = {10.1039/c8re00025e}, author = {Vasudevan, N. and Sharma, Mrityunjay K. and Reddy, D. Srinivasa and Kulkarni, Amol A.} }