A 17 - hydroxy - crag root of beijing euphorbia lactone B synthetic method of
The invention provides a semisynthesis method of 17-hydroxyjolkinolide B. The semisynthesis method comprises the following steps: carrying out a cyclization reaction on a double bond at the C11 position of an epoxy ring of Jolkinolide A serving as a raw material; bromizing a methyl at the C17 position of a lactonic ring, then carrying out debromination and acetylation, and finally hydrolyzing an acetyl to obtain 17-hydroxyjolkinolide B. The invention discloses a new method for synthesizing 17-hydroxyjolkinolide B and provides a basis for research and development of jolkinolide type medicines. The successful synthesis of 17-hydroxyjolkinolide B provides a new direction for research of anti-cancer drugs. The method has the advantages that the yield of 17-hydroxyjolkinolide B can be improved, the production cost can be reduced, the market supply is enlarged and the cancer treatment cost is lowered.
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Paragraph 0038-0039; 0059
(2018/05/16)
Natural crag root of beijing euphorbia lactone Jolkinolide A and B synthetic method
The invention provides a method for synthesizing a jolkinolide A component and a jolkinolide B component which serve as main active components of a traditional Chinese medicine euphorbia fischeriana. The natural jolkinolide A and B is obtained by simple and high-efficiency synthesis through a series of chemical reactions by taking low-cost and readily-available p-13,19-dyhydroxyl kaurene; a preparation condition, a preparation process and important spectral structures and physical property data of all midbodies and target compounds are supplied.
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(2017/08/23)
Efficient Synthesis of Jolkinolides A and B from Steviol
Jolkinolides, isolated from Euphorbia fischeriana Steud, are naturally occurring tetracyclic ent-abietane diterpenes, some of which exhibit promising antitumor and other biological activity. An efficient strategy for the synthesis of jolkinolides A and B is described starting from readily available steviol in 10 and 11 steps with total yields of over 10%, respectively.
TOTAL SYNTHESIS OF (+/-)-JOLKINOLIDE A, B, AND E UTILIZING A NEW MILD ESTERIFICATION FOLLOWED BY INTRAMOLECULAR WITTIG-HORNER REACTION
Jolkinolide A, B, and E were efficiently synthesized from 9-methoxycarbonyl-4,4,10-trimethyl-Δ6-8-octalone 8 through Δ8(14)-podocalpen-13-one 12.A new synthetic method of γ-ylidenbutenolide consisting of mild esterification and the s
Katsumura, Shigeo,Kimura, Akihiko,Isoe, Sachihiko
p. 1337 - 1346
(2007/10/02)
Total Synthesis of (+/-)-Jolkinolide A and B
The first efficient synthesis of jolkinolide A and B from the diosphenol (7) is reported; the new synthetic method described may find use in the preparations of 4-ylidene-2,3-substituted butenolides.
Katsumura, Shigeo,Kimura, Akihiko,Isoe, Sachihiko
p. 330 - 331
(2007/10/02)
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