Toward understanding the scope of Baylis-Hillman reaction: synthesis of 3-(2- hydroxyphenyl)indolin-2-ones and polycyclic fused furans

A facile one-pot synthesis of 3-(2-hydroxyphenyl)indolin-2-ones has been developed via the TiCl₄-mediated Baylis-Hillman (B-H) reaction of N-substituted isatins and cyclohex-2-enone, followed by treatment of the in situ generated B-H alcohols with aq HBr. Baylis-Hillman reaction of aromatic cyclic 1,2-diones with cycloalk-2-enones under the influence of TiCl₄ has been successfully performed and the resulting Baylis-Hillman adducts have been conveniently transformed into pentacyclic and hexacyclic fused furan derivatives.     

An efficient approach to construct 2-arylbenzo[b]furans from 2-methoxychalcone epoxides

An efficient and practical method for construction of 2-arylbenzo[b]furans from 2-methoxychalcone epoxides has been reported. Catalyzed by 2 mol % of BF₃·Et₂O, 2-methoxychalcone epoxides went through the Meerwein rearrangement, followed by deformylation in one-pot to successfully afforded 2-methoxydeoxybenzoins. Afterward, 2-arylbenzo[b]furans were obtained in high yields (87%–100%) via intermolecular cyclodehydration of 2-methoxydeoxybenzoins with 48% HBr. By utilization of this approach, the natural product stemofuran A and the key intermediate of eupomatenoid 6 have been synthesized conveniently.     

Palladium‐Catalyzed Oxidative Cycloisomerization of 2‐Cinnamyl‐1,3‐Dicarbonyls: Synthesis of Functionalized 2‐Benzyl Furans

A new palladium‐catalyzed intramolecular oxidative cycloisomerization of readily available starting materials, 2‐cinnamyl‐1,3‐dicarbonyls, has been demonstrated for the creation of structurally diverse 2‐benzyl furans. The cycloisomerization occurs by a regioselective 5‐exo‐trig pathway. The reaction shows a broad substrate scope with good to excellent yields. Furthermore, a one‐pot procedure has been executed by using readily available cinnamyl alcohols and 1,3‐diketones.     

Synthesis of Highly Substituted 3‐Formylfurans by a Gold(I)‐Catalyzed Oxidation/1,2‐Alkynyl Migration/Cyclization Cascade

3‐Formylfuran derivatives are core structures of a variety of bioactive natural products. However, procedures for their preparation are still rare and generally inefficient in terms of atom economy: These methods require multiple steps or harsh reaction conditions and show selectivity problems. An efficient gold(I)‐catalyzed cascade reaction that leads to 3‐formylfurans from easily accessible starting materials is now described. A wide variety of 3‐formylfurans were obtained from the corresponding symmetric and unsymmetric 1,4‐diyn‐3‐ols in the presence of an N‐oxide in good to excellent yields. Isotope‐labeling experiments as well as DFT calculations support a mechanism in which, after an initial oxygen transfer, a 1,2‐alkynyl migration is favored over a hydride shift; a cyclization ensues to afford the desired functionalized furan core.     

Platinum(II)-Catalyzed Novel Synthesis of 3,4-Fused Furans

A novel synthesis of 3,4-fused furans (both tricyclic and bicyclic) through platinum-catalyzed cyclization of 3-(2-formylcycloalkenyl)-acrylic amides 2 in methanol is described (up to 90% yield). Tricyclic 3,4-fused dihydrofuran derivatives were also obtained via reductive cyclization of 2. The substrates 2 were obtained from β- bromovinyl aldehydes by a Pd-catalyzed Heck reaction.     

壳聚糖酶的研究进展

壳聚糖酶是最近发现的一种专一性降解壳聚糖的新酶。本文概述了壳聚糖酶的分布,理化性质和固定化情况,综述了它的催化降解特异性和分子学研究进展,对它在植物抗性方面的应用作了简要介绍。     

糖基阳离子表面活性剂的研究进展

由糖基开发出的各种阳离子表面活性剂既有糖基非离子表面活性剂的温和性、低毒性、低刺激性、与阴离子表面活性剂良好的配伍性能和协同增效作用,还有阳离子表面活性剂的杀菌性、抗静电性和柔软性等性能,在洗涤剂、医药、化妆品、农业、材料、皮革、造纸和食品等领域具有广阔的应用前景。本文综述了国内外糖基阳离子表面活性剂的合成路线、分子结构和应用领域,并对该领域的研究现状、存在的问题和未来的发展方向进行了讨论与展望。     

A One-Pot Approach to Novel Pyridazine C-Nucleosides

The synthesis of glycosides and modified nucleosides represents a wide research field in organic chemistry. The classical methodology is based on coupling reactions between a glycosyl donor and an acceptor. An alternative strategy for new C-nucleosides is used in this approach, which consists of modifying a pre-existent furyl aglycone. This approach is applied to obtain novel pyridazine C-nucleosides starting with 2- and 3-(ribofuranosyl)furans. It is based on singlet oxygen [4+2] cycloaddition followed by reduction and hydrazine cyclization under neutral conditions. The mild three-step one-pot procedure leads stereoselectively to novel pyridazine C-nucleosides of pharmacological interest. The use of acetyls as protecting groups provides an elegant direct route to a deprotected new pyridazine C-nucleoside.     

含二肽的新型糖基氨基硫脲的合成

由N-苄氧羰基-L-氨基酸与氨基酸甲酯作用,再进一步肼解得到N-苄氧羰基-二肽酰肼。将N-苄氧羰基-二肽酰肼与糖基异硫氰酸酯反应,得到一系列新型的N-糖基-2-（N-苄氧羰基-二肽）-氨基硫脲（1a-11,2a-21,3a-31）。新化合物的结构经IR,^1HNMR,MS谱和元素分析确证。