- 2. 4 - difluorobenzene methylamine synthetic method
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The invention relates to the fields of medicine and agrochemicals, and concretely relates to a synthetic method of an intermediate 2,4-difluorobenzene methylamine. The synthetic method comprises the following steps: 1) m-difluorobenzene, a halogenating agent and paraformaldehyde are reacted under effect of a catalyst to prepare 2,4-difluoro benzyl halide; 2)the prepared 2,4-difluoro benzyl halide and urotropine are reacted to prepare a quaternary ammonium salt compound IV; 3)the prepared quaternary ammonium salt compound is hydrolyzed by concentrated hydrochloric acid to obtain 2,4-difluorobenzene methylamine. The method has the advantages of low cost of the prepared 2,4-difluorobenzene methylamine, convenient operation and high security coefficient, and is suitable for industrial production.
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Paragraph 0036-0040
(2017/10/22)
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- [4,5]-fused-3,6-disubstituted-pyridazines with sulfur-containing substituents in position three for the treatment of neoplasia
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[4,5]-Fused-3,6 disubstituted-pydidazines of Formula I are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia: wherein Y1and Y2are independently selected from the group consisting of (CH2)n,—C(X)—NH—,—(CH2)n—C(X)—O—, and X is O or S; R1is selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, and substituted or unsubstituted phenyl, pyridinyl, and the like; R2is selected from the group consisting of substituted or unsubstituted phenyl, benzyl, pyridinyl, and the like; “A” is a benzene ring fused with the pyridazine ring; and R3is independently selected in each instance form the group consisting of halogen, lower alkyl, and the like.
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