- Improved Preparation of the Clathrate Host Compound Tri-o-thymotide and Related Trisalicylide Derivatives
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In order to improve the relatively low yield (ca. 35percent) previously observed in the synthesis of tri-o-thymotide (TOT, 1) from o-thymotic acid (2), the cyclodehydration was studied using a variety of conditions.The low yield is due to the formation of di-o-thymotide (DOT, 3), previously reported, and at least three other products (4-6), which apparently result from the acid-catalyzed decarboxylation of 2 and subsequent condensation with thymol (7).Using pyridine as a solvent, side-product formation is inhibited.Under appropriate conditions, namely, neat POCl3 at 50 deg C, the yield of 1 is 93percent.Other salicylic acid derivatives also give high yields of the corresponding "trimers" under these conditions, thus providing a general, improved preparation of a family of potential clathrate host substances.
- Gnaim, Jallal M.,Green, Bernard S.,Arad-Yellin, Rina,Keehn, Philip M.
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p. 4525 - 4529
(2007/10/02)
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- Antianaphylactic Benzophenones and Related Compounds
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The synthesis and biological properties of 85 benzophenones and related compounds are described.The majority of the compounds inhibit the release of leukotrienes (LT) C4 and D4 in vitro from sensitized guinea pig chopped lung.In addition, some of the compounds inhibited the release of LTs from passively sensitized human chopped lung and protected guinea pigs from the effects of anaphylaxis in a modified Herxheimer test.
- Evans, Delme,Cracknell, Mark E.,Saunders, John C.,Smith, Christine E.,Williamson, W. R. Nigel,et al.
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p. 1321 - 1327
(2007/10/02)
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