Preparation method of hexahydrofuranofuranol derivative, intermediate and preparation method thereof
The invention relates to the field of medicine synthesis, in particular to a preparation method of a hexahydrofuranofuranol derivative, an intermediate and a preparation method thereof. The preparation method comprises a condensation reaction, a deprotection reaction and a cyclization reaction, wher...
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| creator | ZHENG HUI YE MEIQI LIN JINGXIN LIU SHENGMIN GAO ZHAOBO |
| description | The invention relates to the field of medicine synthesis, in particular to a preparation method of a hexahydrofuranofuranol derivative, an intermediate and a preparation method thereof. The preparation method comprises a condensation reaction, a deprotection reaction and a cyclization reaction, wherein R1 and R2 are hydrogen or hydroxyl protecting groups, R3 is alkyl, acyl, ether, ester or aryl, and X is oxygen, sulfur or nitrogen. In the preparation process of the hexahydrofuranofuranol derivative, the compound shown in the formula I is subjected to a condensation reaction, so that the product with very high optical purity can be prepared by adopting the way. The preparation method can be used for commercially producing and preparing the darunavir key intermediate (3R, 3aS, 6aR)- hexahydrofuro-[2, 3-b]-3-ol, and is a very economical route suitable for industrial production.
本发明涉及医药合成领域，具体涉及六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法。该制备方法包括缩合反应、脱保护、环合反应，其中，R1和R2为氢或羟基保护基，R3为烷基、酰基、醚基、酯基或芳基,X为氧、硫或氮。在六氢呋喃并呋喃醇衍生物的制备过程中，式I化合物通过缩合 |
| format | Patent |
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本发明涉及医药合成领域，具体涉及六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法。该制备方法包括缩合反应、脱保护、环合反应，其中，R1和R2为氢或羟基保护基，R3为烷基、酰基、醚基、酯基或芳基,X为氧、硫或氮。在六氢呋喃并呋喃醇衍生物的制备过程中，式I化合物通过缩合</description><language>chi ; eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2021</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20210202&DB=EPODOC&CC=CN&NR=112300186A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20210202&DB=EPODOC&CC=CN&NR=112300186A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>ZHENG HUI</creatorcontrib><creatorcontrib>YE MEIQI</creatorcontrib><creatorcontrib>LIN JINGXIN</creatorcontrib><creatorcontrib>LIU SHENGMIN</creatorcontrib><creatorcontrib>GAO ZHAOBO</creatorcontrib><title>Preparation method of hexahydrofuranofuranol derivative, intermediate and preparation method thereof</title><description>The invention relates to the field of medicine synthesis, in particular to a preparation method of a hexahydrofuranofuranol derivative, an intermediate and a preparation method thereof. The preparation method comprises a condensation reaction, a deprotection reaction and a cyclization reaction, wherein R1 and R2 are hydrogen or hydroxyl protecting groups, R3 is alkyl, acyl, ether, ester or aryl, and X is oxygen, sulfur or nitrogen. In the preparation process of the hexahydrofuranofuranol derivative, the compound shown in the formula I is subjected to a condensation reaction, so that the product with very high optical purity can be prepared by adopting the way. The preparation method can be used for commercially producing and preparing the darunavir key intermediate (3R, 3aS, 6aR)- hexahydrofuro-[2, 3-b]-3-ol, and is a very economical route suitable for industrial production.
本发明涉及医药合成领域，具体涉及六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法。该制备方法包括缩合反应、脱保护、环合反应，其中，R1和R2为氢或羟基保护基，R3为烷基、酰基、醚基、酯基或芳基,X为氧、硫或氮。在六氢呋喃并呋喃醇衍生物的制备过程中，式I化合物通过缩合</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2021</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjDELwjAUBrM4iPofnrtCY0FcpShO4uBeHuYLCbRJeH0W_fc6dHNxuVuOmxt3ExQW1pgT9dCQHWVPAS8ObyfZP4XTxI4cJI7fdsSGYlJIDxdZQZwcld-TBgiyX5qZ527AavLCrM-ne3PZouQWQ-EHErRtrtbu6qqyh_2x_qf5AKa2QCA</recordid><startdate>20210202</startdate><enddate>20210202</enddate><creator>ZHENG HUI</creator><creator>YE MEIQI</creator><creator>LIN JINGXIN</creator><creator>LIU SHENGMIN</creator><creator>GAO ZHAOBO</creator><scope>EVB</scope></search><sort><creationdate>20210202</creationdate><title>Preparation method of hexahydrofuranofuranol derivative, intermediate and preparation method thereof</title><author>ZHENG HUI ; YE MEIQI ; LIN JINGXIN ; LIU SHENGMIN ; GAO ZHAOBO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN112300186A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>chi ; eng</language><creationdate>2021</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>ZHENG HUI</creatorcontrib><creatorcontrib>YE MEIQI</creatorcontrib><creatorcontrib>LIN JINGXIN</creatorcontrib><creatorcontrib>LIU SHENGMIN</creatorcontrib><creatorcontrib>GAO ZHAOBO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>ZHENG HUI</au><au>YE MEIQI</au><au>LIN JINGXIN</au><au>LIU SHENGMIN</au><au>GAO ZHAOBO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Preparation method of hexahydrofuranofuranol derivative, intermediate and preparation method thereof</title><date>2021-02-02</date><risdate>2021</risdate><abstract>The invention relates to the field of medicine synthesis, in particular to a preparation method of a hexahydrofuranofuranol derivative, an intermediate and a preparation method thereof. The preparation method comprises a condensation reaction, a deprotection reaction and a cyclization reaction, wherein R1 and R2 are hydrogen or hydroxyl protecting groups, R3 is alkyl, acyl, ether, ester or aryl, and X is oxygen, sulfur or nitrogen. In the preparation process of the hexahydrofuranofuranol derivative, the compound shown in the formula I is subjected to a condensation reaction, so that the product with very high optical purity can be prepared by adopting the way. The preparation method can be used for commercially producing and preparing the darunavir key intermediate (3R, 3aS, 6aR)- hexahydrofuro-[2, 3-b]-3-ol, and is a very economical route suitable for industrial production.
本发明涉及医药合成领域，具体涉及六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法。该制备方法包括缩合反应、脱保护、环合反应，其中，R1和R2为氢或羟基保护基，R3为烷基、酰基、醚基、酯基或芳基,X为氧、硫或氮。在六氢呋喃并呋喃醇衍生物的制备过程中，式I化合物通过缩合</abstract><oa>free_for_read</oa></addata></record> |
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| title | Preparation method of hexahydrofuranofuranol derivative, intermediate and preparation method thereof |
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