7-异丙基-4-甲基-1-甲醇的简单甲基化反应及其产物性质研究(英文)

研究了新化合物 7 异丙基 1 甲氧甲基 4 甲基 (1)的合成方法及其物理化学性质。通过 7 异丙基 4 甲基 1 甲醇 (2 )与甲醇之间的简单醚化反应即可以制得化合物 1,比常规醚化的反应条件温和而简单易行 ,仅用乙醚溶剂、无机酸催化剂和 0～ 5℃的反应温度 ,在数分钟内即可完成反应。反应还生成二聚体化合物 (5 )及其它少量多聚体副产物。经过1HNMR ,FTIR ,UV vis ,HR MS等波谱分析证实了新化合物 1和 5的化学结构。     

7—异丙基—4—甲基—1—Yu甲醇的简单甲基化反应及其产物性质研究

研究了新化合物7-异丙基-1-甲氧甲基-4-甲基Yu（1）的合成方法及其物理化学性质。通过7-异丙基-4-甲基-1-Yu甲醇（2）与甲醇之间的简单醚化反应即可能制得化合物1，比学会醚化的反应条件温和而简单易行，仅用乙醚溶剂、无机酸催化剂和0-5℃的反应温度，在数分钟内即可完成反应。反应还生成二聚体化合物（5）及其它少量多聚体副产物。经过^1H NMR，FTIR，UV-vis，HR-MS等波谱分析证实了新化合物1和5的化学结构。     

合成1-(β,γ-环氧丙氧甲基)-7-异丙基-4-甲基反应影响因素探讨

研究了7-异丙基-4-甲基-1-甲醇和环氧氯丙烷在碱性催化条件下反应合成1-(β,γ-环氧丙氧甲基)-7-异丙基-4-甲基这一新化合物的影响因素,结果表明影响反应和得率的主要因素为催化剂、碱浓度、反应温度及反应时间.在浓KOH-H2O溶液、惰性有机溶剂、相转移催化剂、40～80 ℃水浴等反应条件下,反应可在2～3 h内完成,得率达64 %.     

1-(β,γ-环氧丙氧甲基)-7-异丙基-4-甲基的合成及结构鉴定

在相转移催化作用下,将7-异丙基-4-甲基-1-甲醇(2)和环氧氯丙烷进行反应,成功地合成了新的反应型类化合物1-(β,γ-环氧丙氧甲基)-7-异丙基-4-甲基(1).本反应条件比较简单,较佳条件下分离的目的物摩尔得率达到了64%.目的物(1)的化学结构(Fig.2)经过UV-Vis、IR、HR-MS和1H NMR等数据分析得到了完满的鉴定.     

合成1-(β，γ-环氧丙氧甲基)-7-异丙基-4- 甲基反应影响因素探讨

研究了７异丙基４甲基１甲醇和环氧氯丙烷在碱性催化条件下反应合成１（β,γ环氧丙氧甲基）７异丙基４甲基这一新化合物的影响因素,结果表明影响反应和得率的主要因素为催化剂、碱浓度、反应温度及反应时间。在浓ＫＯＨＨ２Ｏ溶液、惰性有机溶剂、相转移催化剂、４０～８０℃水浴等反应条件下,反应可在２～３ｈ内完成,得率达６４％     

合成1—（β,γ—环氧丙氧甲基）—7—异丙基—4—甲基Ao反应影响因素探讨

研究了７－异丙基－４－甲基－１－Ａｏ甲醇和环氧氯丙烷在碱性催化条件下反应合成１－（β，γ－环氧丙氧甲基）－７－异丙基－４－甲基Ａｏ这一新化合物的影响因素，结果表明影响反应和得率的主要因素为催化剂，碱浓度，反应温度及反应时间。     

1-(β,γ-环氧丙氧甲基)-7-异丙基-4-甲基薁的合成及结构鉴定(英文)

在相转移催化作用下，将７异丙基４甲基１甲醇（２）和环氧氯丙烷进行反应，成功地合成了新的反应型类化合物１（β，γ环氧丙氧甲基）７异丙基４甲基（１）。本反应条件比较简单，较佳条件下分离的目的物摩尔得率达到了６４％。目的物（１）的化学结构（Ｆｉｇ．２）经过ＵＶＶｉｓ、ＩＲ、ＨＲＭＳ和１ＨＮＭＲ等数据分析得到了完满的鉴定。     

氨基甲酸酯类化合物的合成及其AChE抑制活性研究

以松节油主要组分3-蒈烯为原料首先合成了3-异丙基-5-甲酚(1)和香芹酚(2),从这2个化合物出发通过异氰酸酯法(方法A)和氨基甲酰氯法(方法B)进一步制备了14个含异丙基甲酚结构的氨基甲酸酯类化合物,并测定了所合成16个化合物对乙酰胆碱脂酶(AChE)的抑制活性。研究结果表明：酚类化合物与异氰酸酯反应是制备氨基甲酸酯的高效合成工艺,其中异氰酸酯中N-取代基结构越大反应越容易发生,芳基取代产物的摩尔得率可达90%以上。在AChE抑制活性方面,3-异丙基-5-甲酚衍生物的抑制活性普遍高于香芹酚衍生物,N-脂基取代产物的抑制活性显著高于N-芳基取代产物,且短链脂基取代产物的抑制活性高于长链脂基和环脂基。3-异丙基-5-甲酚的N-甲基取代产物表现出优良的AChE抑制活性,抑制效率达到石杉碱甲的90.5%,超过同为氨基甲酸酯阳性对照利凡斯的明(89.6%),而其N,N-二甲基取代产物的抑制活性又明显高于N-甲基取代产物,抑制效率达到石杉碱甲的97.9%。浓度与抑制率关系表明：3-异丙基-5-甲基苯基-N,N-二甲基氨基甲酸酯(Ⅰ-2)在浓度大于1.25 mmol/L后表现出与石杉碱甲基本等同...     

四季青中一个新的酚性化合物

对冬青科植物冬青干燥叶(四季青)的化学成分进行了研究.取干药材10 kg, 加8倍量体积分数80 %乙醇回流煎煮3次, 每次4 h,回收乙醇至无醇味.浸膏混悬于适量水中,依次用石油醚、乙酸乙酯、正丁醇萃取,回收溶剂.采用不同层析技术进行分离,从正丁醇部位分得1个酚性化合物,经理化及光谱方法鉴定为:3,4-二羟基 -7-(3′-O-β-D-吡喃葡萄糖基 -4′-羟基 -苯甲酰基) -苯甲醇(俗称四季青酚苷),一种新化合物.     

1—（β,γ—环氧丙氧甲基）—7—异丙基—4—甲基ao的合成及结构鉴定

在相转移催化作用下,将７－异丙基－４－甲－１－ａｏ甲醇（２）和环氧氯丙烷进行反应,成功地合成了新的反应型ａｏ类化合物１－（β,γ－环氧丙氧甲基）－７－异丙基－４－甲基ａｏ（１）。     

对伞花烃直接电解氧化反应的评价

研究了在有机溶剂、合适的支持电解质和碳棒存在下，对伞花烃的直接电解氧化反应，使用GC和GC-MS方法分析测定了主要电解氧化产物，如：百里香酚甲醚、1-异丙基-4-甲氧甲基苯、枯茗醛、枯茗醇、对二甲氧甲基异丙基苯、枯茗酸甲酯、对羟基甲氧甲基异丙基苯、乙酸枯茗酯和1-二甲氧甲基-4-(1-甲氧基-1-甲基乙基)苯。详细研究了影响氧化主产物得率的主要因素，对伞花烃直接电解氧化选择性地制备枯茗醛合理的电解条件为：电解时间20-25h，甲醇／乙酸体积比10：1，氟硼酸钠作支持电解质，阳极／阴极面积比1：1，电流密度0．018A／cm^2。     

Antifungal properties of methanol extract and its active compounds from Brickellia rosmarinifolia Vent

A new isocoumarin, 7-hydroxyl-4-methyl isocoumarine (1), together with three known monoterpenes, (3R, 4R, 6S)-3, 6-dihydroxy-1-menthene (2), (+)-(1R, 3S, 4R, 6S)-6-hydroxymenthol (3) and 4-isopropyl-1-methylcyclohex-2-ene-1, 6-diol (4), was isolated from the methanol extract of Brickellia rosmarinifolia. The structures were determined by spectroscopic means. Compounds 1, 2, 3 and 4 showed antifungal activities against Colletotrichum musae and Peronophythora litchii in vitro.     

Diarylheptanoids from the rhizomes of Alpinia officinarum and their anticancer activity

Two new diarylheptanoids (1, 2), together with two known analogs (3, 4), were isolated from the rhizomes of Alpinia officinarum. The new compounds were elucidated to be (5S)-5-hydroxy-7-(3, 4-dihydroxyphenyl)-1-phenyl-3-heptanone (1) and (5R)-5-hydroxy-7-(3-methoxy-4, 5-dihydroxyphenyl)-1-phenyl-3-heptanone (2) based on their spectral analysis. Compound 4 showed moderate cytotoxicity against human tumor cell lines, HepG2, MCF-7 and SF-268, while no significant effect were found for compounds 1-3.     

A novel xanthene from Indigofera longeracemosa stem

A novel xanthene, 3-isopropyl-9a-methyl-1,2,4a,9a-tetrahydroxanthene (1), was isolated from the stem of Indigofera longeracemosa.     

Constituents of Agave americana and Agave barbadensis

An investigation of Agave americana and Agave barbadensis resulted in the isolation of a new homoisoflavanoid, 7-hydroxy-3-(4-methoxybenzyl)-chroman (3), together with known compounds 7-hydroxy-3-(4-methoxybenzyl)-chroman-4-one (1), 5,7-dihydroxy-3-(4-methoxybenzyl)-chroman-4-one (2), cantalasaponin-1 (4), and 2-hydroxy-butanedioic acid-1-methyl ester (5).     

In vivo antidepressant activity of sesquiterpenes from the roots of Valeriana fauriei Briq

Antidepressant activity-guided fractionation of the MeOH extract of Valeriana fauriei Briq. roots resulted in the isolation of two new germacrane-type sesquiterpenes (1-2) in addition to seven known ones (3-9). Their structures were elucidated as 1β,10α-dihydroxyl-8α-acetoxyl-10β,11,11-trimethyl-4-formyl-bicyclogermacren-E-4(5)-ene (1), 1β-hydroxyl-8α-acetoxyl-11,11-dimethyl-4-formyl-bicyclogermacren-E-4(5),10(14)-diene (2), bicyclo[8,1,0]5β-hydroxyl-7β-1acetoxyl-5α,11,11'-trimethyl -E-1(10)-ene-4α,15-olide (3), 8α-acetoxyl-3α,4α,10-trihydroxyl-guaia-1(2)-ene-12,6α-olide (4), 2-Ethylhexyl-4-hydroxybenzoate (5), 11αH-gemacra-1(10)E,4Z-diene-3-one-12,6α-olide (6), β-Sitoterol (7), isovaleric acid (8), isoborneol acetate (9), using a combination of UV, IR, mass spectroscopy, 1D and 2D NMR spectroscopy. The antidepressant activity of compounds 1-4 was investigated by the FST on mice. Among them, compounds 3 and 4 showed the significant antidepressant activity (*, P<0.01).     

Further degradation product of hyperforin from Hypericum perforatum (St John's Wort)

Repeated examination of the aerial parts of Hypericum perforatum yielded a new degradation product of hyperforin (1) namely deoxyfurohyperforin A (2), together with the previously identified furohyperforin (3), furoadhyperforin (4), furohyperforin A (5a and 5b), pyrano[7,28-b]hyperforin (6) and 3-methyl-4,6-di(3-methyl-2-butenyl)-2-(2-methyl-1-oxopropyl)-3-(4-methyl-3-pentenyl)-cyclohexanone (7). The antimicrobial activity of the compounds 3, 5a and 5b, 6 and 7 was tested against Staphylococcus aureus, Candida albicans, Bacillus subtilis and Escherichia coli.     

New cytotoxic quinolone alkaloids from fruits of Evodia rutaecarpa

Three new quinolone alkaloids, 1-methyl-2-[7-hydroxy-(E)-9-tridecenyl]-4(1H)-quinolone (1), 1-methyl-2-[(Z)-4-nonenyl]-4(1H)-quinolone (2), 1-methyl-2-[(1E,5Z)-1,5-undecadienyl]-4(1H)-quinolone (3) and one new natural product, 1-methyl-2-[(E)-1-undecenyl]-4(1H)-quinolone (4), were isolated from the dried and nearly ripe fruits of Evodia rutaecarpa (Juss.) Benth., along with thirteen known compounds (5-17). In addition, one new artificial product, 1-methyl-2-[7-carbonyl-(E)-9-tridecenyl]-4(1H)-quinolone (1A) was also obtained. The structures of these compounds were determined by spectroscopic analyses. The cytotoxic activities of all of the compounds against the human cancer cell lines HL-60, N-87, H-460, and Hep G(2) cells were evaluated by MTT assay. The results showed that these alkaloids inhibited cell proliferation with IC(50) values between 14μM and 22μM.