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A kind of preparation method of pharmaceutical intermediate

An intermediate and pharmaceutical technology, applied in the field of chemical and pharmaceutical intermediates, to achieve the effects of cheap and easy-to-obtain raw materials, novel synthetic routes, and simple operations

Active Publication Date: 2021-05-04
SHAOXING UNIVERSITY
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Problems solved by technology

It has been speculated that perhaps thousands of species of endophytes are of great importance to humans, but due to few researchers working in this field and deforestation, many useful endophytes may be discovered in their medicinal uses value is gone forever

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  • A kind of preparation method of pharmaceutical intermediate

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[0026] The present invention starts from the raw material (R)-epichlorohydrin, and provides a pharmaceutical intermediate (S)-1-[(4S,5R)-4-(2,2 - a preparation method of dimethyl-5E-propenyl-1,3-dioxol (1,3-dioxol)]-1-octanol (1), which comprises 8 steps of reaction in total.

[0027] (a) Preparation of (R)-1-chloro-5-trimethylsilyl-4-pentyn-2-alcohol:

[0028] Under anhydrous and oxygen-free conditions, dissolve trimethylsilylacetylene (5.82g, 0.06mol) in anhydrous tetrahydrofuran (250mL), add butyllithium (2.5M, 24mL, 0.06mol) dropwise at minus 78 degrees, and stir After 1 hour, add boron trifluoride diethyl ether (0.06mol), and after 10 minutes, add the raw material R-epichlorohydrin (4.85g, 0.05mol), keep the temperature for 2 hours, then raise the temperature to minus 30 degrees, and keep the reaction for 19 After 1 hour, TLC detected that the reaction of the raw materials was complete, adding saturated ammonium chloride to quench the reaction, distilling off the solvent...

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Abstract

The invention discloses a preparation method of a pharmaceutical intermediate, whose chemical name is: (S)-1-[(4S,5R)-4-(2,2-dimethyl-5 E ‑propenyl‑1,3 dioxolane]‑1‑octanol, which belongs to the field of chemical and pharmaceutical intermediates. The present invention starts from the chiral raw material (R)-epichlorohydrin, and the preparation process needs to go through reduction reaction, prins cyclization reaction, asymmetric dihydroxylation reaction, elimination reaction participated by zinc powder and double bond isomerization catalyzed by rhodium Reaction and so on 8-step reaction. The invention has the advantages of simple operation, cheap and easy-to-obtain raw materials, novel synthesis route, high-efficiency construction of multiple chiral centers, and the like.

Description

technical field [0001] The invention belongs to the field of chemical and pharmaceutical intermediates, in particular to a pharmaceutical intermediate (S)-1-[(4S,5R)-4-(2,2-dimethyl-5E-propenyl-1,3-dioxy Preparation method of cyclopentyl]-1-octanol (1). Background technique [0002] The breadth and diversity of secondary metabolites produced by endophytes have been shown to be useful against pathogens and even cancers in animals, including humans. It has been speculated that perhaps thousands of species of endophytes are of great importance to humans, but due to few researchers working in this field and deforestation, many useful endophytes may be discovered in their medicinal uses The value is gone forever. It is worth mentioning that endophytic fungi isolated from Amazonian tropical plants are rich sources of important medicinal secondary metabolites. Polyhydroxyl structures are ubiquitous in many natural products or drug molecules and intermediates. Among the many seco...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D317/20
Inventor 杨震张梦帆王翔叶青青
Owner SHAOXING UNIVERSITY
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