双环缩酮类信息素——Brevicomin和Fmntalin合成研究进展

介绍了双环缩酮类信息素——Brevicomin和Frontalin在立体选择性和非立体选择性合成中的各种方法。参考文献48篇。     

桃柱螟性信息素的立体选择性合成

分别以10-十一碳烯酸和丙炔醇为起始原料,通过炔化物路线(第1个中间体是10-十一碳炔醇-1(5),第2个中间体是10-十六碳炔醇-1(8))分别立体选择性合成了桃柱螟性信息素成分(E)-10-十六碳烯醛(1)和(Z)-10-十六碳烯醛(2)。     

苄基酒石酸甲乙酯的立体选择性合成

本文报道了赤式苄基酒石酸甲乙酯(3)的立体选择性合成,其~1H核磁共振谱、红外光谱和质谱与预期的结构一致。这个方法对合成其它具有赤式酒石酸结构的天然产物有一定的参考价值。     

β—咔啉及吲哚喹嗪生物碱类似物的立体选择性合成

自然界吲哚生物碱种类繁多,结构复杂,生物活性明确而又重要。吲哚生物碱的消炎、止泻、平喘、止咳、降压、兴奋中枢神经,乃至抗肿瘤等药理作用,在临床上被广泛应用。剖析结构,它们中有相当数量化合物与β-咔啉(β-     

可交联嘌呤类脱氧核苷类似物的合成

可交联嘌呤类脱氧核苷是天然脱氧核苷类似物,可与互补链中配对碱基上的胺基发生链间交联反应,导致DNA双链发生不可逆转的交联,对开发核苷类药物和控制修饰基因表达等方面有重要应用。本文开发了一条新的合成路径,该方法以商业化的1-氯-2-脱氧-3,5-二-O-对甲苯甲酰基-D-呋喃核糖为起始原料,经由简便的合成路线制备了目标产...     

烯基溴化合物的合成方法研究进展

以烯基溴化合物为代表的烯基卤代烃(1-卤代-1-烯烃)是过渡金属催化下通过C—C偶联反应构建多取代烯烃的重要合成砌块.因此,开发简便、有效的合成烯基溴化合物的新方法越来越受到人们的重视和关注.对按照所使用的合成原料进行分类,对近年来所报道的烯基溴化合物的合成方法进行了回顾.所综述的主要的合成方法中所涉及的合成原料涵盖了酮类、炔类、炔丙醇类、烯基三氟甲磺酸酯类、3-芳基-2,3-二溴丙酸、苄基溴类、丙烯酸类、环丙烯类和烯丙醇类衍生物等共9类化合物.     

红霉素合成的进展

红霉素合成的成就,标志着立体选择合成效率的进步。本文评述红霉素化学合成的进展     

紫杉醇的合成进展

紫杉醇是一种重要的抗癌药物,它具有复杂新颖的化学结构,为三环二萜类化合物.本文综述了紫杉醇的半合成和紫杉烷环的各种合成方法.     

MK-287类PAF拮抗剂的合成

以(±)-4,10-二氧杂三环[5,2,1,0^2,6]-癸-8-烯-3-醇和PhTi(OPr-i)₃为原料,经过芳基化、氧化、芳基化、环化、热分解和加氢反应,高立体选择性地合成了反式-2,5-二芳基四氢呋喃.     

经由胂叶立德立体有择合成仿保幼激素──增丝素（ZR－512）及其（2Z，4E）－异构体

３－甲基－２－丁烯酸乙酯４经ＳｅＯ２反式氧化、还原、溴化得到关键中间体４－溴－３－甲基－（２Ｅ）－丁烯酸乙酯７．７与三苯基胂反应生成季８．二氢香茅醛与８在Ｋ＿２ＣＯ＿３－乙醇－微量水的存在下反应，得到（２Ｅ，４Ｅ）－３，７，１１－三甲基－２，４－十二碳二烯酸乙酯１ａ及其（２Ｚ，４Ｅ）－异构体１ｂ，产率７４％。该反应具有（４Ｅ）－立体选择性，同时Ｃ－２双键发生部分构型转化。     

酰胺类化合物的高效合成研究

酰胺类化合物是有机化学中最常见的化合物之一, 在药物化学、生物化学以及高分子合成等领域都有着重要的应用. 近年来高效合成酰胺类化合物已经成为一个研究热点, 具有重要的意义.本文主要从过渡金属催化、有机小分子催化等方面讨论近几年来酰胺类化合物的合成研究进展, 并对其发展趋势进行展望.     

Synthesis of flavonoid 2-deoxyglucosides via the Mitsunobu reaction

The Mitsunobu reaction of flavonoids and 3,4,6-tri-O-acetyl-2-deoxy-d-glucopyranose or 3,4,6-tri-O-benzyl-2-deoxy-d-glucopyranose is a very effective method for the stereoselective synthesis of flavonoid 2-deoxyglucosides. Since there is no C2 substituent on the sugar moieties, the observed α- or β-stereoselectivity was mainly controlled by the (acetyl or benzyl) protecting groups. Possible mechanistic insights are offered to explain the dual stereoselectivity.     

New Radical Route and Insight for the Highly Efficient Synthesis of Benzimidazoles Integrated with Hydrogen Evolution

Benzimidazoles are a versatile class of scaffolds with important biological activities, whereas their synthesis in a lower-cost and more efficient manner remains a challenge. Here, we demonstrate a conceptually new radical route for the high-performance photoredox coupling of alcohols and diamines to synthesize benzimidazoles along with stoichiometric hydrogen (H₂) over Pd-decorated ultrathin ZnO nanosheets (Pd/ZnO NSs). The mechanistic study reveals the unique advantage of ZnO NSs over other supports and particularly that the features of Pd nanoparticles in facilitating the cleavage of the α-C−H bond of alcohols and adsorbing subsequently-generated C-centered radicals hold the key to turning on the reaction. This work highlights a new insight into radical-induced efficient benzimidazole synthesis pairing with H₂ evolution by rationally designing semiconductor-based photoredox systems.     

An Efficient Synthesis of Dicyclohexylmethyl Diazoacetate

Oiazoacetateisaversatilereagentinorganicsynthesis'.Ithasbeenwidelyusedincyclopropanation.etheration.elc.Bothenantiomericselectivityanddiastereoselectivit}ofcyclopropanationaregreatlyaffectedbyalkylgroupofalkyldiazoacetate.Highselectivitieswereobtainedusingstericdemandingdiazoacetate.Aratallihasusedmenth}'jdiazoacetate(MnDA)=.andDoylehasemployed2.6-di-lerl-butyl-4meth\lphenyldiazoacetate3toachievehighselectivities.Masamunefoundthatdicyclohexylmethyldiazoacetate(DCHMDA)wassuperiortotheabove…     

Modulation of the stereoselectivity and reactivity of glycosylation via (p-Tol)2SO/Tf2O preactivation strategy: From O-, C-sialylation to general O-, N-glycosylation

We make a review on the progress of the (p-Tol)₂SO/Tf₂O preactivation strategy for general glycosylation using thioglycosides or sialyl sulfoxide as donors.     

Highly Efficient Synthesis of the Natural Spiro-Terpenoid ( ± )-Andirolactone via RCM Reaction

Andirolactone 1 as the dextro enantiomer is a sesquiterpenoid with structure of spirocyclic butenolide, isolated from the wood of cedar ( Cedrus libanotica ), which is a needle-leaf tree that grows in southern Turkey and Libanon.The tar, which is obtained from its wood, is used to cure various diseases. [1]     

核苷研究（Ⅳ）：辛可芬三唑啉硫酮核苷的立体选择性合成

核苷研究（Ⅳ）──辛可芬三唑啉硫酮核苷的立体选择性合成陈宏明，张键，毛建民，蔡孟深（北京医科大学药学院有机教研室，北京，１０００８３）关键词核苷，合成，立体选择性辛可芬（Ｃｉｎｃｈｏｐｈｅｎ）早年作为镇痛药和抗炎症药曾被广泛应用于临床［１］，由于它有...