1,1—二甲基—7—异丙基—1,2,3,4—四氢萘—6—磺酸钠的合成

文章探讨了１，１－二甲基－７－异丙基－１，２，３，４－四氢萘－６－磺酸钠合成的磺化工艺。通过实验室的试验，确定了适宜的工艺条件，１，１－二甲基－７－惜内基－１，２，３，４，－四四氢萘与浓度硫酸的配比为１：１０．５（ｍｏｌ比），反应温度９０±２℃，反应时间２０ｍｉｎ，产品得率达８０．３％。同时测定了产物表面活性性能，可用作表面活性剂。     

2,6—二甲基—7—辛烯—2—烷基（或羟烷基）醚的合成研究

以氢型丝是石为催化剂，二氢月桂烯与单醇或二醇加成反应生成２，６－二甲基＝７－辛烯－２－烷基或烃烷基醚。实验结果发现，各种醇与烯生成醚化合物的趋势如下；直链伯醇易于支链伯醇；伯醇易于仲醇；低碳直链伯醇易于高碳直链伯醇，同时还发现，１，３－丁二、１，６－己二椁民烯的反应，只生成单醚。文中还考察了反应温度和时间对反应的影响。     

异冰片基氧丙酮及4—异冰片基氧—2—丁酮的合成

将莰烯分别与１，２－丙二醇及１，３－丁二醇加成所得产物１－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］２－丙醇及４－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］－２－丁醇，氧化得到两只新型的可用作香料的萜醚酮，１－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］丙酮，与４－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］－２－丁酮。     

两种臭灵丹精油成分的比较研究

从六棱臭灵丹和臭灵丹两种鲜叶分别提取的精油分析表明，其成分和含量不同，六棱菊中有较高含量的４－甲基「３、１、０」双环己烷（１６．８２），１－辛烯３－醇（２．３２％）桉叶油素（１．８９％），「３、７、１１」－三甲基－「１、６、１０」－十二三烯－３－醇）３．０４％）。     

异冰片基氧丙酮及4－异冰片基氧－2－丁酮的合成

将莰烯分别与１，２－丙二醇及１，３－丁二醇加成所得产物１－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］２－丙醇及４－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］－２－丁醇，氧化得到两只新型的可用作香料的萜醚酮，１－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］丙酮，与４－［（１，７，７－三甲基双环［２，２，１］庚－２－基）氧］－２－丁酮。     

α—蒎烯合成杀虫增效剂的研究

松节油的主要成分α－蒎烯经异构同时与马来酸酐发生Ｄｉｅｌｓ－Ａｌｄｅｒ反应，生成１－异丙基－４－甲基二环「２，２，２」－５－辛烯－２，３－二羧酸酐。研究影响反应的主要因素：加料顺序，催化剂和助催化剂用量，原料配比，反应时间和反应温度等，得出比较适宜的反应条件。     

日本落叶松林分生长和收获预估模型的研究

本文根据影响林分生长的主要因子，林龄、地位指数和林分密度，以多因子综合描述的方法，采用Ｈ优１．３＋ｂ１ＳＩｂ２（１－ｅ－ｂ３Ａｔ）ｂ４ＳＩｂ５＋ε、ＳＩ＝ｂ１Ｈ优ｂ２（１－ｅ－ｂ３Ａｔ）ｂ４Ｈ优－ｂ５＋ε和增加密度指标的Ｙ＝ｂ１ＳＩｂ２（１－ｅ－ｂ３Ｎｂ４ｔ）ｂ５；收获预估采用布伦德和科拉特的ｌｏｇＣＶ＝ｂ１＋ｂ２ＳＩ＋ｂ３（１／Ａ２）＋ｂ４（１－Ａ１／Ａ２）＋ｂ５（ｌｏｇＢ）（Ａ１／Ａ２），建立日本落叶松林分生长和收获预估模型。精度验证该组模型基本满足要求。同时又据辽宁省栽培的日本落叶松早期生长受冻干危害的特点，引入了胸高年龄的概念，提高了模型的精度。     

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）。     

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。     

苯基异氰酸酯在N,N—二甲替乙酰胺中的副反应

本文研究了异氰酸基在Ｎ，Ｎ－二甲替乙酰胺中的副反应，虽然４，４－二苯基甲烷二氰酸酯在ＤＭＡＣ中很稳定，且在３℃时不发生任何反应，但在４０℃时，异氰酸基的含量逐渐减少，以致最后形成凝胶。用苯基异氰酸酯作为ＭＤＩ的模型化合物，进行ＰＩ在ＤＭＡＣ中副反应产物的鉴定研究，鉴定出以下五种副反应产物；（１）１，３－二苯基脲（ＤＰＵ）；（２）１，３－二苯基－５－苯胺甲酰基－６－二甲胺基尿嘧啶（ＰＵＲ）；（３）１     

Ent-trachyloban-19-oic acid isolated from Iostephane heterophylla as a promising antibacterial agent against Streptococcus mutans biofilms

From the roots of Iostephane heterophylla, six known compounds, namely, ent-trachyloban-19-oic acid (1), the mixture of ent-kaur-16-en-19-oic acid (2) and ent-beyer-15-en-19-oic acid (3), xanthorrhizol (4), 16α-hydroxy-ent-kaurane (5) and 16α-hydroxy-ent-kaur-11-en-19-oic acid (6) were isolated using a bioassay-guided fractionation method. The known compounds (1-6) were identified by comparison of their spectroscopic data with reported values in the literature. In an attempt to increase the resultant antimicrobial activity of 1 and 4, a series of reactions was performed on ent-trachyloban-19-oic acid (1) and xanthorrhizol (4), to obtain derivatives 1a, 1b, and 4a-4d. All the isolated compounds (1-6) and the derivatives 1a, 1b, and 4a-4d were evaluated for their antimicrobial activity against two oral pathogens, Streptococcus mutans and Porphyromonas gingivalis associated with caries and periodontal disease, respectively. Compounds 1, 1b, 2+3, 4 and 4d inhibited the growth of S. mutans with concentrations ranging from 4.1 μg/mL to 70.5 μg/mL. No significant activity was found on P. gingivalis except for 4 with an MIC of 6.8 μg/mL. The ability of 1, 1b, 2+3, 4 and 4d to inhibit biofilm formation by S. mutans was evaluated. It was found that 1, 1b, 4 and 4d interfered with the establishment of S. mutans biofilms, inhibiting their development at 32.5, 125.0, 14.1 and 24.4 μg/mL, respectively.     

Heptaketides with antiviral activity from three endolichenic fungal strains Nigrospora sp., Alternaria sp. and Phialophora sp

Two new heptaketides, (+)-(2S,3S,4aS)-altenuene (1a) and (-)-(2S,3S,4aR)-isoaltenuene (2a), together with six known compounds, (-)-(2R,3R,4aR)-altenuene (1b), (+)-(2R,3R,4aS)-isoaltenuene (2b), 5'-methoxy-6-methyl-biphenyl-3,4,3'-triol (3), alternariol (4), alternariol-9-methyl ether (5), and 4-hydroxyalternariol-9-methyl ether (6) were isolated from the EtOAc extract of an endolichenic fungal strain Nigrospora sphaerica (No.83-1-1-2). Compounds 1a and 1b were separated from enantiomers 1 by chiral HPLC, and so were 2a and 2b from enantiomers 2. Interestingly, 1-6 were also obtained from other two endolichenic fungal strains Alternaria alternata (No.58-8-4-1) and Phialophora sp. (No.96-1-8-1). The structures of 1-6 were elucidated by means of MS, HR-MS, NMR, and X-ray diffraction. Furthermore, the absolute configurations of 1a-2b were determined by CD experiments and CD calculation. Of these compounds, 4 and 5 showed antiviral activity against herpes simplex virus (HSV) in vitro, with IC(50) values of 13.5 and 21.3 μM, and with selective index (SI) values of 26.5 and 17.1, respectively.     

Antileishmanial polyphenols from Garcinia vieillardii

Seven xanthones, the new vieillardiixanthones B and C (1) and (7), pancixanthones A (2), B (3), 1,6-dihydroxyxanthone (6), pyranojacareubin and 5,6-O-dimethyl-2-deprenylrheediaxanthone together with two benzophenones, clusiachromene (4) and 3-geranyl-2,4,6-trihydroxybenzophenone (5) were isolated from the stem bark of the neocaledonian Garcinia vieillardii. 2, 5 and 6 showed a significant antileishmanial activity against the promastigote forms of Leishmania mexicana and L. infantum and against the amastigote forms of L. infantum.     

新型脱氢枞胺1,2,3-噻二唑衍生物的合成及表征

以脱氢枞胺为原料,在三氟乙酸酐和乙酸酐保护其氨基后,经B环铬酸氧化转化成为(酮)N-三氟乙酰基-7-氧代脱氢枞胺(2a)和N-乙酰基-7-氧代脱氢枞胺(2b),酮再与盐酸氨基脲缩合形成(缩氨基脲)N-三氟乙酰基脱氢枞胺-7-氨基脲酰腙(3a)和N-乙酰基脱氢枞胺-7-氨基脲酰腙(3b),然后在氯化亚砜的处理下发生Hurd-Mori反应,环合生成(B环并1,2,3-噻二唑衍生物)N-三氟乙酰基脱氢枞胺-6-烯[7,6-d]-并-1,2,3-噻二唑(4a)和N-乙酰基脱氢枞胺-6-烯[7,6-d]-并-1,2,3-噻二唑(4b),最后在碱性条件下水解脱去氨基保护基,合成了脱氢枞胺-6-烯[7,6-d]-并-1,2,3-噻二唑(5)。通过FT-IR、~1H NMR、~(13) C NMR和ESI-MS等方法对2a、3a、4a、4b和5的结构进行了表征,进一步分析了4a、4b和5这3种新型脱氢枞胺1,2,3-噻二唑衍生物的谱图特征及结构差异。     

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.     

In vitro anti-uveal melanoma activity of phenolic compounds from the Egyptian medicinal plant Acacia nilotica

Anti-uveal melanoma activity-guided fractionation of the MeOH extract of Acacia nilotica pods resulted in the isolation of the new compound gallocatechin 5-O-gallate (5) in addition to methyl gallate (1), gallic acid (2), catechin (3), catechin 5-O-gallate (4), 1-O-galloyl-β-D-glucose (6), 1,6-di-O-galloyl-β-D-glucose (7) and digallic acid (8). The structures of the isolated compounds were elucidated on the basis of HRESIMS, NMR spectroscopy and CD data. In addition to uveal melanoma, the antiproliferative activities of the isolated compounds and the related compound epigallocatechin 3-O-gallate (EGCG) were evaluated against cutaneous melanoma, ovarian cancer, glioblastoma and normal retinal pigmented cells.     

Potent and selective butyrylcholinesterase inhibitors from Ficus foveolata

Four stilbenes (1-4), one inseparable mixture of two alkyl diferulates (5a, 5b), one alkyl ferulate (6) and four flavonoids (7-10) were isolated from Ficus foveolata Wall. Except for quercetin (10), the other ten constituents were isolated from F. foveolata for the first time. In addition, one of the two components in mixture 5 is a new compound identified as (1E,22E)-1,22-docosanediol diferulate (5a). All nine isolated compounds, plus the mixture of 5a and 5b known as 5, exhibited a low or no activity against acetylcholinesterase. However, and interestingly, the stilbenes 1-4 showed a high inhibition towards butyrylcholinesterase. Gnetol (4) had the lowest IC(50) value of 1.3μM towards butyrylcholinesterase and showed a reversible and competitive inhibition in the kinetic study.     

高效液相色谱-电喷雾质谱联用分析喜树果鞣花酸类成分

建立喜树果的液相色谱质谱联用分析方法,并分析了喜树果中的鞣花酸类化合物。大孔吸附树脂分离、HPLC–ESI–(MS)n数据分析结果:初步分析到5个化合物,即3,4-O,O-亚甲基-3’,4’-O-二甲基鞣花酸、3’-O-甲基鞣花酸-4’-O-葡萄糖苷、鞣花酸-4’-O-鼠李糖苷、3,4’-O-二甲基鞣花酸、3,3’4,4’-O-四甲基-5’-甲氧基鞣花酸。用HPLC–ESI–(MS)n方法分析喜树果鞣花酸类成分,方便、快捷、实用。     

Phenolics from Bidens bipinnata and their amylase inhibitory properties

A new chlorinated flavonoid, 3, 6, 8-trichloro-5, 7, 3', 4'-tetrahydroxyflavone (1), a new biscoumaric acid derivative, 4-O-(2″, 3″-O-diacetyl-6″-O-p-coumaroyl-β-d-glucopyranosyl)-p-coumaric acid (2), and 8, 3', 4'-trihydroxyflavone-7-O-β-d-glucopyranoside (3) together with twenty-four known compounds (4-27) were isolated from the whole plant of Bidens bipinnata. All chemical structures were established on the basis of UV-, MS- and NMR ((1)H, (13)C, (1)H-(1)H COSY, HMQC and HMBC) spectroscopic data. Some of the isolated compounds were tested for the inhibition of α-amylase. The result showed that isookanin (6) was a potent inhibitor of α-amylase (IC(50)=0.447mg/ml).