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An effcient synthetic protocol for the β-amino carbonyl compounds was developed via one-pot three-component Mannich reaction of aromatic aldehydes, aromatic amines and cyclohexanone catalyzed by 2-hydroxylpy-ridine under mild reaction conditions. β-Amino carbonyl compounds were obtained in moderate to good yields and reasonable diastereoselectivities. The effects of different solvents, catalyst amounts and the scope of different substrates on the Mannich reactions were investigated. The plausible reaction mechanism was also discussed. 相似文献
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IntroductionInrecentyears ,dihydropyrimidinethionederivativeshaveattractedconsiderableinterestduetotheirpromisingactivitiesasanticarcinogenicagents ,1cardiovasculara gents2 andcalciumchannelblockers .3Inaddition ,somederivativesofdihydropyrimidinethionewer… 相似文献
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Direct Catalytic Asymmetric Mannich Reaction with Dithiomalonates as Excellent Mannich Donors: Organocatalytic Synthesis of (R)‐Sitagliptin 下载免费PDF全文
Dr. Han Yong Bae Mun Jong Kim Jae Hun Sim Prof. Dr. Choong Eui Song 《Angewandte Chemie (International ed. in English)》2016,55(36):10825-10829
In this study, dithiomalonates (DTMs) were demonstrated to be exceptionally efficient Mannich donors in terms of reactivity and stereoselectivity in cinchona‐based‐squaramide‐catalyzed enantioselective Mannich reactions of diverse imines or α‐amidosulfones as imine surrogates. Owing to the superior reactivity of DTMs as compared to conventional malonates, the catalyst loading could be reduced to 0.1 mol % without the erosion of enantioselectivity (up to 99 % ee). Furthermore, by the use of a DTM, even some highly challenging primary alkyl α‐amidosulfones were smoothly converted into the desired adducts with excellent enantioselectivity (up to 97 % ee), whereas the use of a malonate or monothiomalonate resulted in no reaction under identical conditions. The synthetic utility of the chiral Mannich adducts obtained from primary alkyl substrates was highlighted by the organocatalytic, coupling‐reagent‐free synthesis of the antidiabetic drug (?)‐(R)‐sitagliptin. 相似文献
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Ga(ClO4)3-catalyzed reaction of 1,2-aryldiamines and α-bromoketones to afford 2-substituted quinoxa- lines in good yields is described. The reaction proceeded via grinding process with 10%(molar fraction) catalyst under solvent-free conditions at room temperature. For unsymmetrical o-phenylenediamines bearing electron-with- drawing groups, regio-selective quinoxalines were obtained. 相似文献
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In the presence of catalytic amount of In(OTf)3 (10 mol%), a series of aldimines reacted with tetraallyltin in a 2:1 molar ratio to afford the corresponding homoallylic amines in good yields. The good atom efficiency was achieved under mild reaction conditions and a new protocol (allyl)4Sn/In(OTf)3 for simple imines was developed. 相似文献
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O,O'Diethyl acetals were prepared in high yields under mild conditions via the reaction of triethyl orthoformate with aldehydes and ketones in absolute ethanol in the presence of as low as 0.1 tool% of Yb(OTf)3. Using the same catalyst in THF-H2O, these O,O'-diethyl acetals could be converted to the corresponding carbonyl compounds efficiently. This new protection-deprotection protocol presents the advantages of ease of execution, high efficiency and good chemoselectivity. 相似文献
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Zhen-Zhen Chen Dong-Zhao Yang Ying-Ying Dong Mei Chi Shou-Zhi Pu Qi Sun 《Molecules (Basel, Switzerland)》2022,27(3)
Hafnium(IV) triflate (Hf(OTf)4) has been identified as a potent catalyst for the direct three-component synthesis of β-carbamate ketones. This new method, featuring a low catalyst loading, fast reaction rate, and solvent-free conditions, provided facile access to a diversity of carbamate-protected Mannich bases. A mechanistic investigation indicated that the three-component reaction proceeds via sequential aldol condensation and aza-Michael addition, but not the Mannich-type pathway. 相似文献
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Rina Ghosh Swarupananda Maiti Arijit Chakraborty Dilip K. Maiti 《Journal of molecular catalysis. A, Chemical》2004,210(1-2):53-57
A new efficient one-pot synthesis of α-amino phosphonates derived from nitro substituted anilines, aldehydes and diethyl phosphite has been carried out by employing 5 mol% of In(OTf)3. The method is equally effective for the generation of α-amino phosphonates from various carbonyl compounds and other amines. 相似文献
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A general and practical procedure for the syntheses of 3,4-di-hydropyrimidine-2(1H)-thiones by a one-pot condensation of aldehyde,β-ketoester or β-diketone and thiourea using La(OTf)3 as the catalyst is described.Mild reaction conditions,excellent yields as well as the environmentally friendly character of La(OTf)3 make it an important alternative to the classic acid-catalyzed Biginelli‘s reaction. 相似文献
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合成了14个含1,2-环己二胺、1,2-二苯基乙二胺或邻苯二胺的手性Salen化合物, 研究了手性Salen直接催化苯基锂对环氧环己烷的不对称开环反应, 结果表明二胺的结构和苯环上3,3'-位取代基对反应的对映选择性有很大的影响. 用Salen与 Me3Ga原位生成的Ga(Salen)催化苯基锂对环氧环己烷的不对称开环反应, 与用Salen直接催化相比, 得到了更好的化学产率和对映选择性. 当用Ga(Slane) 15为催化剂时, 最佳ee值为73%. 相似文献