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Oxazolyl steroid derivative as well as synthesis method and application thereof

A technology of oxazolyl steroids and derivatives, which is applied in the field of drug synthesis, can solve the problems of yield and quality loss, and achieve the effect of high production yield and easy separation

Active Publication Date: 2021-02-19
NORTHWEST A & F UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Piercing-sucking pests are one of the most serious pests in agriculture. For example, aphids and whiteflies can harm most crops, causing serious losses to their yield and quality. However, after long-term use of effective control agents, many Most have developed severe resistance to piercing-sucking pests

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  • Oxazolyl steroid derivative as well as synthesis method and application thereof
  • Oxazolyl steroid derivative as well as synthesis method and application thereof
  • Oxazolyl steroid derivative as well as synthesis method and application thereof

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Embodiment Construction

[0028] In the following, the technical solution of the present invention will be described in conjunction with examples, but the present invention is not limited to the following examples.

[0029] Synthesis and preparation of the oxazolyl steroid derivatives of the present invention. Its synthesis idea can be divided into three parts: the first part, first react dehydroepiandrosterone 1 with N,N-dimethylformamide, tert-butyldimethylchlorosilane to protect the three-position hydroxyl of 1, and then tetrahydrofuran As a solvent, ethyltriphenylphosphine bromide and potassium tert-butoxide were added to obtain compound 3, and finally asymmetric dihydroxylation reaction occurred under the catalysis of AD-mix-bata to obtain compound 4; the second part, with various acid chlorides As the reaction raw material, a hydrazinolysis reaction occurs in the case of ethanol as a solvent to obtain 6c-31c, and then dichloromethane is used as a solvent to close the ring in the presence of triet...

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Abstract

The present invention provides an oxazolyl steroid derivative having a chemical structure represented by general formula (1) shown in the specification, wherein a substituent R represents one of an alkyl group, a phenyl group or a substituted phenyl group. The invention further provides a synthesis method of the oxazolyl steroid derivative. Biological assay proves that the oxazolyl steroid derivative has good poisoning activity on piercing-sucking insects such as eriosoma lanigerum, myzus persicae, yellow aphid and whiteflies, and can be used for preventing and controlling plant insect pests.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and relates to an oxazolyl steroid derivative, in particular to the preparation of the oxazolyl steroid derivative and its application in the control of diseases and insect pests. Background technique [0002] Heterocyclic compounds are ubiquitous in nature and widely used, and occupy a very important position in people's real life. The vast majority of drugs and more than half of organic compounds are heterocyclic compounds. The synthesis of heterocyclic compounds and the exploration of their biological activities are one of the important research fields of organic chemistry, medicinal chemistry and pesticide development, especially some heterocyclic compounds containing N and O heteroatoms have shown good bactericidal activity. It has been widely used in pesticide, medicine and other fields. [0003] Oxazole compounds in nitrogen-containing heterocyclic rings are one of the more ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00A01N45/02A01P7/04
CPCC07J43/003A01N45/02
Inventor 师宝君马世闯李奇蒋伟奇吴文君
Owner NORTHWEST A & F UNIV
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