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Abstract
Graphical Abstract Section
Abstract
Synth. Commun. 2007, 37, 9
SYNTHESIS OF β-SECRETASE INHIBITORS CONTAINING A HYDROXYETHYLENE DIPEPTIDE ISOSTERE
Xiaoming Yang, Xiaomin Zou, Yiqiu Fu, Ke Mou, Gang Fu, Chao Ma, and Ping Xu
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing, China
A new β-secretase inhibito 17 was synthesized via two pathways, with detailed discussion and comparison of respective reation conditions and yields.
Abstract
Synth. Commun. 2007, 37, 25
L -PROLINE-PROMOTED CuI-CATALYZED C-S BOND FORMATION BETWEEN ARYL IODIDES AND THIOLS
Hui Zhang,1 Weiguo Cao,1,2 and Dawei Ma3
1Department of Chemistry, Shanghai University, Shanghai, China
2State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Science, Shanghai, China
3State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Science, Shanghai, China
An improved, mild procedure for the CuI-catalyzed coupling reactions of aryl iodides with aliphatic and aromatic thiols, using L-proline as the ligand, is reported.
Abstract
Synth. Commun. 2007, 37, 37
FACILE AND EFFICIENT WAY TO SYNTHESIZE THE RADICAL CYCLIZATION PRECURSOR METHYL 3-(TERT-BUTYL((E)-3-(2,2-DIPHENYLCYCLOPROPYL)-2-PROPENYL)AMINO)-3-OXO-2-(PHENYLSELENO)PROPANOATE FOR KINETIC RESEARCH
Jindi Yu, Gaoyan Lian, and Danwei Zhang
Department of Chemistry, Fudan University, Shanghai, China
Abstract
Synth. Commun. 2007, 37, 47
EFFICIENT BIGINELLI REACTION CATALYZED BY SULFAMIC ACID OR SILICA SULFURIC ACID UNDER SOLVENT-FREE CONDITIONS
Wei-Yi Chen,1 Su-Dong Qin,2 and Jian-Rong Jin1
1College of Chemistry and Chemical Engineering of Suzhou University, Suzhou, China
2Technical Department of JiangShan Pharmaceutical Corporation, JingJiang, China
Sulfamic acid efficiently catalyzes the three-component condensation reaction of aldehydes, 1,3-dicarbonyl compounds, and urea/thiourea under solvent-free conditions to afford the corresponding dihydropyrimidinones and thio-derivatives in high yields. Silica sulfuric acid is also found to be an efficient catalyst for the Biginelli reaction under solvent-free conditions. Compared to the classical Biginelli reaction conditions, this new method consistently has the advantage of giving good yields and requiring short reaction times.
Abstract
Synth. Commun. 2007, 37, 53
NEW STRAIGHTFORWARD SYNTHESIS OF 2-AMINO-6-METHYL-5-(PYRIDIN-4-YLSULFANYL)-3H-QUINAZOLIN-4-ONE
Wei-Min Chen,1,2 and Shan-He Wan2
1Department of Medicinal Chemistry, School of Pharmacy, Jinan University, Guangzhou, China
2Institute of Pharmaceutical Sciences, First Military Medical University, Guangzhou, China
2-Amino-6-methyl-5-(pyridin-4-ylsulfanyl)-3H-quinazolin-4-one (1) was synthesized with 2-guanidino-5-bromo-6-methylquinazolin-4-one (6) as the key intermediate in a one-pot synthesis by treatment of compound 6 with 4-mercaptopyridine and KOH. 4-Mercaptopyridine was found to play the role of protecting agent to prevent -Br on a quinazoline ring from being substituted by -OH.
Abstract
Synth. Commun. 2007, 37, 63
CONCISE AND EFFICIENT SYNTHESIS OF LINEAR FUROCOUMARINS: PSORALEN AND 4-METHYLPSORALEN
Bang-Le Zhang,1,2 Fang-Dao Wang,1 and Jian-Min Yue1
1State Key Laboratory of Drug Research, Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, China
2School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi, China
A method for the rapid synthesis of psoralen and 4-methylpsoralen has been developed. The key intermediates, coumarinyloxyaldehydes, were obtained in only two steps from the easily available starting materials, 7-hydroxycoumarin derivatives, by an oxidative procedure. Using Swern oxidation, psoralen and 4-methylpsoralen were finally produced in the overall yields of 71% and 67%, respectively.
Abstract
Synth. Commun. 2007, 37, 71
SYNTHESIS AND STRUCTURE OF NOVEL DISULFIDE(TRISULFIDE)-CONTAINING THIOPHENES
Shi-Ren Deng,1 Tao Wu,2 Gao-Qiang Hu,1 Dan Li,2 Yun-Hong Zhou,1 and Zao-Ying Li1
1Department of Chemistry, Wuhan University, Wuhan, China
2Department of Chemistry, Shantou University, Shantou, China
Abstract
Synth. Commun. 2007, 37, 79
DESIGN AND SYNTHESES OF NOVEL CALIX[4](AZA)CROWNS: NEUTRAL RECEPTORS FOR α‐AMINO ACIDS
Fafu Yang,1 Yanqing Ji,1 Hongyu Guo,1 Jianrong Lin,1 and Qi Peng2
1College of Chemistry and Materials Science, Fujian Normal University, Fuzhou, China
2State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou, China
Series of novel calix[4](aza)crowns 2a–2d countaining acylhydrazone groups were synthesized and showed good complexation abilities towards α-amino acids.
Abstract
Synth. Commun. 2007, 37, 87
EFFICIENT α-CHLORINATION AND α-BROMINATION OF CARBONYL COMPOUNDS USING N-HALOSUCCINIMIDES/UHP IN IONIC LIQUID
Jong Chan Lee and Hyun Jung Park
Department of Chemistry, Chung-Ang University, Seoul, South Korea
A novel method is developed for the transformation of aryl ketones into their corresponding α-haloaryl ketones using NXS and UHP in [bmim]BF4
Abstract
Synth. Commun. 2007, 37, 91
L-PROLINE-CATALYZED MICHAEL ADDITION OF ALDEHYDES AND UNMODIFIED KETONES TO NITRO OLEFINS ACCELERATED BY Et3N
B. M. Choudary,1 Ch. V. Rajasekhar,2 G. Gopi Krishna,2 and K. Rajender Reddy2
1Ogene Systems (I) Pvt. Ltd., Hyderabad, India
2Inorganic and Physical Chemistry Division, Indian Institute of Chemical Technology, Hyderabad, India
Abstract
Synth. Commun. 2007, 37, 99
INTRAMOLECULAR AMIDATION: SYNTHESIS OF NOVEL THIAZOLE-FUSED DIAZEPINONES
Rajesh S. Koti, Gundurao D. Kolavi, Vinayak S. Hegde, and Imtiyaz Ahmed M. Khazi
Department of Chemistry, Karnatak University, Dharwad, India
A new fused heterocycile system, thiazolodiazepinone, is synthesized by applying intramolecular hydrazonolysis to 2-coumarinyl-5-formylthiazole.
Abstract
Synth. Commun. 2007, 37, 107
A SIMPLE AND CONVENIENT SYNTHESIS OF PYRAZINONES
Saikat Das Sharma, Pranjal Gogoi, and Dilip Konwar
Synthetic Organic Chemistry Division, Regional Research Laboratory, Jorhat, Assam, India
Abstract
Synth. Commun. 2007, 37, 113
REACTION OF β‐LAPACHONE WITH 1,2‐DIAMINES: FACILE SYNTHESIS OF NOVEL TETRACYCLIC PYRAZINES
Pahup Singh,1 Anshu Dandia,1 Kavita Natani,1 Venu Sharma,1 Raju Ratnani,2 A. L. Bingham,3 M. B. Hursthouse,3 M. E. Light,3 and J. E. Drake4
1Department of Chemistry, University of Rajasthan, Jaipur 302004 India
2Department of Pure and Applied Chemistry, M.D.S. University, Ajmer, India
3Department of Chemistry, University of Southampton, Highfield, Southampton, United Kingdom
4Department of Chemistry and Biochemistry, University of Windsor, Windsor, Ontario, Canada
Abstract
Synth. Commun. 2007, 37, 119
FACILE SOLID-PHASE SYNTHESIS OF CYCLOALKYLPHOSPHONATES AND 1-CYCLOALKENYLPHOSPHONATES USING POLYMER-SUPPORTED PHENYLSULFONYLMETHYLPHOSPHONATES
Xiao-Ling Liu, Shou-Ri Sheng, Wei Zhou, Qiu-Ying Wang, Xiao-Lan Zhang, and Bin Gong
College of Chemistry and Chemical Engineering, Jiangxi Normal University, Nanchang, China
A facile procedure for the solid-phase synthesis of cycloalkylphosphonates and 1-cycloalkenylphosphonates in good yields and high purities using polystyrene-supported phenylsulfonylmethylphosphonates with traceless sulfone linker strategy is described.
Abstract
Synth. Commun. 2007, 37, 129
CONVENIENT SYNTHESIS OF AN N-(1-ALKOXYL-9-FLUORENYL)SERINE ACRIDINE CONJUGATE
Jifeng Dai and Qibing Zhou
Department of Chemistry, Virginia Commonwealth University, Richmond, Virginia, USA
Abstract
Synth. Commun. 2007, 37, 137
HALOGENATION OF PYRAZOLES USING N-HALOSUCCINIMIDES IN CCL4 AND IN WATER
Zhi-Gang Zhao and Zhong-Xia Wang
Department of Chemistry, University of Science and Technology of China, Hefei, Anhui, China
Reaction of pyrazoles with N-halosuccinimides (NXS, X=Cl, Br) in CCl4 or water gave 4-halopyrazoles in excellent yields. The reaction was carried out under mild conditions and did not require any catalysts or special precautions.
Abstract
Synth. Commun. 2007, 37, 149
TRANSFORMATION OF ARYL ACYLOIN O-ALKYL AND O-PHENYL DERIVATIVES TO KETONES
Zhiyi Yao,1 Deju Ye,1 Hong Liu,1 Kaixian Chen,1 and Hualiang Jian1,2
1Center for Drug Discovery and Design, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, and Graduate School, Chinese Academy of Sciences, Shanghai, China
2School of Pharmacy, East China University of Science and Technology, Shanghai, China
The treatment of aryl acyloin (α-hydroxyketone) O-alkyl and O-phenyl derivatives with 2–3 equiv of Zn and 1–2 equiv of NH4Cl in ethanol, refluxing for 20–120min, gave the corresponding ketones with excellent yields. Further, α,β-epoxy ketones can be efficiently transformed to β-hydroxy ketones, and 2,2-dialkoxy-1-phenyl ketone also can be dealkoxylated to 1-phenyl ketone.
Abstract
Synth. Commun. 2007, 37, 157
SYNTHESIS OF NOVEL NORCANTHARIDIN DERIVATIVES OF SUBSTITUTED AROMATIC AMINES WITH IMPROVED 1,3‐DIPOLAR CYCLOADDITION
Liping Deng and Yongzhou Hu
Zhejiang University, Department of Medicinal Chemistry, School of Pharmaceutical Science, Hangzhou, China
