- Method for preparing mepanipyrim
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The invention provides a preparation method of mepanipyrim and belongs to the field of pesticide chemical synthesis technologies. The preparation method of the mepanipyrim comprises the following steps: firstly, reacting phenyl guanidine salt with ethyl acetoacetate so as to prepare phenylamino pyrimidone, reacting the phenylamino pyrimidone with phosphorus oxychloride so as to prepare 2-chloro-pyrimidine phenylamine; subsequently, carrying out coupling and crossing reaction between the 2-chloro-pyrimidine phenylamine and alkyne so as to prepare mepanipyrim. The preparation method of mepanipyrim has the advantages that the used raw materials and reagents are cheap and easily available; the reaction process is simple, the reaction conditions are mild, the cost is low, the yield is high, a good condition is created for industrial large-scale production and commercialization of the products.
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Paragraph 0014; 0015; 0020; 0025
(2018/07/30)
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- Synthesis of novel thiazolyl-pyrimidines and their anticancer activity in vitro
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A series of novel compounds 7-43 were prepared via the condensation of enaminones 4a-h and the guanidines carbonate 6a-f. The structures of these newly synthesized compounds were confirmed by 1H-NMR, MS, EA and IR. All the compounds were tested for their cytotoxic activity in vitro against human cancer cell lines including Ishikawa, A549, BEL-7404, SPC-A-01 and SGC-7901. Most of them showed moderate cytotoxic against the tested cell lines. Among them, the most potent compounds 9 and 30 exhibited more efficient activity against Ishikawa, A549. Thiazolyl-pyrimidines were synthesized by the general pyrimidine condensation of Bredereck and their in-vitro anticancer activities were evaluated. Copyright
- Shi, Hai-Bo,Li, Hai-Bo,Lu, Kong-Qin,Zhu, Xia-Re,Hu, Wei-Xiao,Pei, Wen
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scheme or table
p. 675 - 683
(2012/06/01)
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- Substituted benzene derivatives useful as neuraminidase inhibitors
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A compound of the Formula (I): STR1 or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1; m is 0; p is 0-1; R1 is --CO2 H; R2 is selected from the group consisting of H, --OH, and --NH2 ; R3 is H; R4 is --C(O)NHR8 ; R5 is --NHC(R6)NH2 R6 is selected from the group consisting of =NH, =NOH, =NCN, =O, and =S; and R8 is selected from the group consisting of C1 -C4 linear or branched alkyl substituted with 0-3 halogens on each carbon.
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- Process for the production of guanidine derivatives
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A process for the production of phenylguanidine carbonate and hydrogencarbonate by reacting aqueous cyanamide with aniline hydrochloride within a specified pH range, combining the reaction mixture with an alkali metal carbonate or hydrogencarbonate, and separating the crystalline product.
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