Enzymatic synthesis and phosphorolysis of 4(2)-thioxo- and 6(5)-azapyrimidine nucleosides by E. coli nucleoside phosphorylases

• Vladimir A. Stepchenko,
• Anatoly I. Miroshnikov,
• Frank Seela and
• Igor A. Mikhailopulo

Beilstein J. Org. Chem. 2016, 12, 2588–2601, doi:10.3762/bjoc.12.254

• pioneering works of Friedkin and co-workers (testing of 5-amino- and halogeno derivatives of uracil for TP from horse liver) and Heidelberger and co-workers (practical synthesis of 5-fluoro- and 5-trifluoromethyl-2'-deoxyurines) substrate properties of 5-substituted uracil derivatives were studied in a

A novel and practical asymmetric synthesis of dapoxetine hydrochloride

• Yijun Zhu,
• Zhenren Liu,
• Hongyan Li,
• Deyong Ye and
• Weicheng Zhou

Beilstein J. Org. Chem. 2015, 11, 2641–2645, doi:10.3762/bjoc.11.283

• route for the synthesis of (S)-dapoxetine (1) through this chiral auxiliary. Results and Discussion Herein, a novel and practical synthesis of 1 (Scheme 1) based on (S)-tert-butanesulfinamide (2) was developed. 3-(Naphthalen-1-yloxy)-1-phenylpropan-1-one (3), which was commercially available from J&K

Recent advances in copper-catalyzed asymmetric coupling reactions

• Fengtao Zhou and
• Qian Cai

Beilstein J. Org. Chem. 2015, 11, 2600–2615, doi:10.3762/bjoc.11.280

• coupling The biaryl motif is a key subunit in many natural products and axially chiral ligands. The classical Ullmann coupling is one of the most important methods for the practical synthesis of biaryls [14]. However, only few reports of an asymmetric version of the Ullmann coupling have been documented

Radical-mediated dehydrative preparation of cyclic imides using (NH₄)₂S₂O₈–DMSO: application to the synthesis of vernakalant

• Dnyaneshwar N. Garad,
• Subhash D. Tanpure and
• Santosh B. Mhaske

Beilstein J. Org. Chem. 2015, 11, 1008–1016, doi:10.3762/bjoc.11.113

• for a practical synthesis of vernakalant. Keywords: APS-DMSO; imides; practical synthesis; radical-mediated; vernakalant; Introduction Cyclic imides are privileged pharmacophores and important building blocks for the synthesis of natural products, drugs, agrochemicals, advanced materials and

• developed protocol is wide and pure products could be obtained without column chromatographic purification, which makes it a commercially sustainable process. A practical synthesis of the drug vernakalant has been achieved using our one-pot imide forming process as one of the important steps. Currently, we

• (OAc)2 (10 mol %), ammonium persulfate (APS) (2 equiv), 1,4-dioxane (0.1 M), DMSO (5% v/v), 100 °C, 3 h in a Schlenk tube). A practical synthesis of vernakalant (11). Optimization studiesa. Imides from substituted/unsubstituted aromatic amines and succinic anhydridesa. Imides from substituted

Synthesis of dinucleoside acylphosphonites by phosphonodiamidite chemistry and investigation of phosphorus epimerization

• William H. Hersh

Beilstein J. Org. Chem. 2015, 11, 184–191, doi:10.3762/bjoc.11.19

• interference has also been described [24]. We recently reported the synthesis of a number of chiral disulfide sulfurizing reagents [25] and the results of the sulfurization of phosphite triesters in order to look for stereoselectivity [26]. In order to change such a method into a practical synthesis route for

Practical synthesis of aryl-2-methyl-3-butyn-2-ols from aryl bromides via conventional and decarboxylative copper-free Sonogashira coupling reactions

• Andrea Caporale,
• Stefano Tartaggia,
• Andrea Castellin and
• Ottorino De Lucchi

Beilstein J. Org. Chem. 2014, 10, 384–393, doi:10.3762/bjoc.10.36

A practical synthesis of long-chain iso-fatty acids (iso-C₁₂–C₁₉) and related natural products

• Mark B. Richardson and
• Spencer J. Williams

Beilstein J. Org. Chem. 2013, 9, 1807–1812, doi:10.3762/bjoc.9.210

• from Xanthomonas campestris pv. vesicatoria 85-10 [71]. A direct one step synthesis of 33 was achieved in 51% yield by Wacker oxidation using Pd/O2 [72] of the alkene 22, intercepted from the synthesis of the iso-C15 acid 4. Conclusion We have accomplished a highly practical synthesis of the homologous

Practical synthesis of indoles and benzofurans in water using a heterogeneous bimetallic catalyst

• Cybille Rossy,
• Eric Fouquet and
• François-Xavier Felpin

Beilstein J. Org. Chem. 2013, 9, 1426–1431, doi:10.3762/bjoc.9.160

Study on the total synthesis of velbanamine: Chemoselective dioxygenation of alkenes with PIFA via a stop-and-flow strategy

• Huili Liu,
• Kuan Zheng,
• Xiang Lu,
• Xiaoxia Wang and
• Ran Hong

Beilstein J. Org. Chem. 2013, 9, 983–990, doi:10.3762/bjoc.9.113

• reported in spite of several synthetic efforts toward the core structure [17][18][19][20][21][22][23][24]. The practical synthesis of velbanamine (2) and a general approach toward structurally related alkaloids remain an intriguing task in the synthetic community. Here, we would like to disclose our recent

New simple synthesis of ring-fused 4-alkyl-4H-3,1-benzothiazine-2-thiones: Direct formation from carbon disulfide and (E)-3-(2-aminoaryl)acrylates or (E)-3-(2-aminoaryl)acrylonitriles

• Qiuping Ding,
• Yuqing Lin,
• Guangni Ding,
• Fumin Liao,
• Xiaoyan Sang and
• Yi-Yuan Peng

Beilstein J. Org. Chem. 2013, 9, 460–466, doi:10.3762/bjoc.9.49

• of novel natural-product-like compounds [18][19][20][21][22], we recently reported the practical synthesis of 2-mercapto-4-benzylidene-4H-benzo[d][1,3]thiazines starting from 2-alkynylbenzenamines with CS2, and further transformations to highly functionalized 4-benzylidene-4H-benzo[d][1,3]thiazines

Expanding the chemical diversity of spirooxindoles via alkylative pyridine dearomatization

• Chunhui Dai,
• Bo Liang and
• Corey R. J. Stephenson

Beilstein J. Org. Chem. 2012, 8, 986–993, doi:10.3762/bjoc.8.111

• Chunhui Dai Bo Liang Corey R. J. Stephenson Department of Chemistry and Center for Chemical Methodology and Library Development (CMLD-BU), Boston University, 590 Commonwealth Avenue, Boston, Massachusetts 02215, USA 10.3762/bjoc.8.111 Abstract A mild and practical synthesis of spirooxindole [1,3

Pd/C- Mediated synthesis of indoles in water

• Mohosin Layek,
• Udaya Lakshmi,
• Dipak Kalita,
• Deepak K. Barange,
• Aminul Islam,
• K. Mukkanti and
• Manojit Pal

Beilstein J. Org. Chem. 2009, 5, No. 46, doi:10.3762/bjoc.5.46

• . Conclusions In conclusion, we have demonstrated the potential of our previously reported palladium on carbon mediated practical synthesis of 2-substituted indoles in water. Besides preparing a wide variety of indole derivatives the methodology was utilized to prepare one of our target indole derivatives

Acid- mediated reactions under microfluidic conditions: A new strategy for practical synthesis of biofunctional natural products

• Katsunori Tanaka and
• Koichi Fukase

Beilstein J. Org. Chem. 2009, 5, No. 40, doi:10.3762/bjoc.5.40

• benzylidene acetal groups, and dehydration, which are the keys to the practical synthesis of N-glycans and the immunostimulating natural product, pristane. A distinctly different reactivity from that in conventional batch stirring was found; the vigorous micromixing of the reactants with the concentrated

• ; microfluidic reactions can offer a direct and practical route to the desired compounds without the usual scale-up problems associated with mixing efficiency and the temperature control. They can therefore be regarded as one of the new strategies for the practical synthesis, or in favorable cases, the

Zeolite catalyzed solvent- free one-pot synthesis of dihydropyrimidin- 2(1H)-ones – A practical synthesis of monastrol

• Mukund G. Kulkarni,
• Sanjay W. Chavhan,
• Mahadev P. Shinde,
• Dnyaneshwar D. Gaikwad,
• Ajit S. Borhade,
• Attrimuni P. Dhondge,
• Yunnus B. Shaikh,
• Vijay B. Ningdale,
• Mayur P. Desai and
• Deekshaputra R. Birhade

Beilstein J. Org. Chem. 2009, 5, No. 4, doi:10.3762/bjoc.5.4

Synthesis of imidazol- 1-yl-acetic acid hydrochloride: A key intermediate for zoledronic acid

• Santosh Kumar Singh,
• Narendra Manne,
• Purna Chandra Ray and
• Manojit Pal

Beilstein J. Org. Chem. 2008, 4, No. 42, doi:10.3762/bjoc.4.42

• Santosh Kumar Singh Narendra Manne Purna Chandra Ray Manojit Pal New Drug Discovery, Matrix Laboratories Limited, Anrich Industrial Estate, Bollaram, Jinnaram Mandal, Medak District, Andhra Pradesh, India-502 325. 10.3762/bjoc.4.42 Abstract A convenient and practical synthesis of imidazol-1-yl

A practical synthesis of the ¹³C/¹⁵N- labelled tripeptide N-formyl- Met-Leu-Phe, useful as a reference in solid- state NMR spectroscopy

• Sven T. Breitung,
• Jakob J. Lopez,
• Gerd Dürner,
• Clemens Glaubitz,
• Michael W. Göbel and
• Marcel Suhartono

Beilstein J. Org. Chem. 2008, 4, No. 35, doi:10.3762/bjoc.4.35

• carried out after cleavage from the resin with liquid hydrogen fluoride [11][12]. No experimental procedures were given in all subsequent publications. In this work, we present for the first time in detail an improved practical synthesis for fully 13C/15N-labelled f-MLF-OH (1) based on the Fmoc-strategy

• in the Supporting Information. Supporting Information File 16: A practical synthesis of the 13C/15N-labelled tripeptide N-Formyl-Met-Leu-Phe, useful as a reference in solid-state NMR spectroscopy. Acknowledgements M.S. is grateful for a predoctoral fellowship from the Dr. Hilmer Foundation.

Synthesis of (S)-1-(2-chloroacetyl)pyrrolidine- 2-carbonitrile: A key intermediate for dipeptidyl peptidase IV inhibitors

• Santosh K. Singh,
• Narendra Manne and
• Manojit Pal

Beilstein J. Org. Chem. 2008, 4, No. 20, doi:10.3762/bjoc.4.20

• Santosh K. Singh Narendra Manne Manojit Pal New Drug Discovery, Matrix Laboratories Limited, Anrich Industrial Estate, Bollaram, Jinnaram Mandal, Medak Dist., Andhra Pradesh, India-502 325 10.3762/bjoc.4.20 Abstract An alternative and practical synthesis of (S)-1-(2-chloroacetyl)pyrrolidine-2