- 2-(aminomethyl)thiazolyl-5-nitrile and synthesis method thereof
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The invention belongs to the technical field of organic synthesis, and relates to 2-(aminomethyl)thiazolyl-5-nitrile and a synthesis method thereof. The method comprises the following steps: by takingaminoacetonitrile hydrochloride as a raw material, carrying out eight steps of reactions including substitution, amination, substitution, amination, Boc addition reaction, substitution, substitutionand Boc removal reaction to prepare the 2-(aminomethyl)thiazolyl-5-nitrile. An efficient synthesis method is provided for synthesis of the compound.
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Paragraph 0008; 0025-0027; 0042-0044; 0059-0061
(2020/11/12)
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- Reactions of β-diketone compounds with nitriles catalyzed by Lewis acids: A simple approach to β-enaminone synthesis
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Aluminium chloride selectively promoted the nucleophilic attack of β-diketone compounds with nitriles to give enaminones. Moreover a plausible mechanism for this transformation was given.
- Cheng, Xu,Pei, Shuchen,Xue, Chenchen,Cao, Kaifei,Hai, Li,Wu, Yong
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p. 63897 - 63900
(2015/02/19)
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- The synthesis and evaluation of flavone and isoflavone chimeras of novobiocin and derrubone
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The natural products novobiocin and derrubone have both demonstrated Hsp90 inhibition and structure-activity relationships have been established for each scaffold. Given these compounds share several key structural features, we hypothesized that incorporation of elements from each could provide insight to structural features important for Hsp90 inhibition. Thus, chimeric analogues of novobiocin and derrubone were constructed and evaluated. These studies confirmed that the functionality present at the 3-position of the isoflavone plays a critical role in determining Hsp90 inhibition and suggests that the bicyclic ring system present in both novobiocin and derrubone do not share similar modes of binding.
- Mays, Jared R.,Hill, Stephanie A.,Moyers, Justin T.,Blagg, Brian S.J.
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experimental part
p. 249 - 266
(2010/04/05)
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- New thiazole derivatives as potent and selective 5-hydroxytriptamine 3 (5-HT3) receptor agonists for the treatment of constipation
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The syntheses and biological evaluation of a series of novel indeno[1,2-d]thiazole derivatives are described. Several groups reported 5-HT3 receptor agonists which were mainly evaluated for their activities on the von Bezold-Jarisch reflex (B-J reflex). We discovered that tetrahydrothiazolopyridine derivative 1b had a contractile effect on the isolated guinea pig colon with weak B-J reflex. Our efforts to find a new type of 5-HT3 receptor agonists on the isolated guinea pig colon focused on the synthesis of a fused thiazole derivative 1d modified from 1b and reverse-fused thiazole derivatives (7-10). In this series, 10f (YM-31636) showed high affinity and selectivity for the cloned human 5-HT3 receptor; furthermore, it showed potent and selective 5-HT3 receptor agonistic activity. YM-31636 was examined for its effects on defecation in animals, thus evaluating the compound as an agent against constipation.
- Imanishi, Naoki,Iwaoka, Kiyoshi,Koshio, Hiroyuki,Nagashima, Shin-Ya,Kazuta, Ken-Ichi,Ohta, Mitsuaki,Sakamoto, Shuichi,Ito, Hiroyuki,Akuzawa, Shinobu,Kiso, Tetsuo,Tsukamoto, Shin-Ichi,Mase, Toshiyasu
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p. 1493 - 1502
(2007/10/03)
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