CAS: 264234-05-1; (R,E)-4-((6,7-Dihydroxy-3,7-Dimethyloct-2-En-1-yl)Oxy)-7H-Furo[3,2-G]Chromen-7-One

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CAS号486-60-2 香柑醇； 5-羟基-6,7-呋喃并香豆素

📜6',7'-Dihydroxybergamottin octanal Acetal 反应生成6',7'-二羟薄荷素
参考文献:葡萄柚皮油中的次要呋喃香豆素和香豆素可作为人类细胞色素p450 3A4的抑制剂
标题:葡萄柚皮油中的次要呋喃香豆素和香豆素可作为人类细胞色素p450 3A4的抑制剂
摘要:一种新的环状缩醛(1 Marmin的)(6',7'-二羟基-7-Geranyloxycoumarin),两个新的环状缩醛(5,6 6)',7'-Dihydroxybergamottin,和已知化合物marmin(2),从柚子皮油中分离出7-香叶烷氧基香豆素(3),佛手柑(4)和6',7'-二羟基佛手柑(7).测试了所有化合物对肠道细胞色素p450 3A4的抑制活性,肠道细胞色素p450 3A4是一种参与人体"葡萄柚/药物"相互作用的酶.香豆素(1-3)显示出可忽略的抑制活性,而呋喃香豆素(4-7)显示出强大的体外抑制活性,Ic 50值分别为2.42,0.13,0.27和1.58μm.
Doi:10.1021/np900266M

专利信息

专利号:US-6613918-B1
优先权日:2000-10-20
标 题 :Synthesis of spiro ortho esters, spiro ortho carbonates, and intermediates
发明人：SEEMAYER ROBERT; LIANG JACK
权利人:BIOAVAILABILITY SYSTEMS LLC
摘要:Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

专利号:WO-2004037827-A1
优先权日:2000-10-20
标题 :Synthesis of spiro ortho esters, spiro ortho carbonates, and intermediates

专利号:US-6160006-A
优先权日:1996-10-18
标 题 :6',7'-dihydroxybergamottin, a cytochrome P450 inhibitor in grapefruit
发明人：EDWARDS DAVID J; WOSTER PATRICK M
权利人:UNIV WAYNE STATE
摘要:The present invention provides a composition and methods for inhibiting cytochrome P450 enzyme activity and in particular, inhibiting the activity of the cytochrome P450 3A sub-family of enzymes, specifically, CYP3A4. The present invention provides 6',7'-dihydroxybergamottin, a furanocoumarin, as the compound primarily responsible for the inhibitory effects of grapefruit juice on cytochrome P450 enzyme activity. The present invention also provides a novel synthesis scheme for 6',7'-dihydroxybergamottin.