Efficiency Eff_syn of complex syntheses as multicomponent reactions, its algorithm and calculations based on concrete criteria

• Heiner Eckert

Beilstein J. Org. Chem. 2019, 15, 1425–1433, doi:10.3762/bjoc.15.142

• Heiner Eckert Technical University of Munich, Department of Chemistry, Lichtenbergstr. 4, D-85747 Garching, Germany 10.3762/bjoc.15.142 Abstract A synthesis efficiency algorithm, which must be based on concrete and reliable criteria, is essential for the evaluation and control of complex chemical

• synthesis, notably multicomponent reactions (MCRs). An algorithm has been developed to precisely evaluate even highly complex syntheses with regards to their synthesis efficiency Effsyn as a tool for strict compliance with green chemistry requirements, and for economic progress. The mathematical operations

• are highly suitable for electronic data processing (EDP). This algorithm is also suitable as a basis for fair cost assessment of complex chemical syntheses. Keywords: efficiency; efficiency algorithm; multicomponent; overall yield; synthesis algorithm; synthesis efficiency; synthesis evaluation

Efficient catenane synthesis by cucurbit[6]uril-mediated azide–alkyne cycloaddition

• Antony Wing Hung Ng,
• Chi-Chung Yee,
• Kai Wang and
• Ho Yu Au-Yeung

Beilstein J. Org. Chem. 2018, 14, 1846–1853, doi:10.3762/bjoc.14.158

• isomers such as the non-interlocked products or lower-order catenanes will form, which are detrimental to the synthesis efficiency as well as complicating the purification process [13][14][15][16][17][18][19]. One strategy to overcome this challenge is to couple the mechanical bond and covalent bond

Peptide synthesis: ball-milling, in solution, or on solid support, what is the best strategy?

• Ophélie Maurin,
• Pascal Verdié,
• Gilles Subra,
• Frédéric Lamaty,
• Jean Martinez and
• Thomas-Xavier Métro

Beilstein J. Org. Chem. 2017, 13, 2087–2093, doi:10.3762/bjoc.13.206

• deprotection step, the synthesis efficiency in the BM and in solution was compared based both on the isolated yields and on the purity of the peptides that were assessed by HPLC analysis (Table 1). For all coupling reactions without exception, the yields obtained under BM conditions were higher than that

A quadruple cascade protocol for the one-pot synthesis of fully-substituted hexahydroisoindolinones from simple substrates

• Hong-Bo Zhang,
• Yong-Chun Luo,
• Xiu-Qin Hu,
• Yong-Min Liang and
• Peng-Fei Xu

Beilstein J. Org. Chem. 2016, 12, 253–259, doi:10.3762/bjoc.12.27

• ][21][22][23][24][25][26][27][28][29][30][31][32][33]. By simplifying the experimental procedures and reducing the usage of both solvents and reagents, one-pot reactions can improve the synthesis efficiency and both save time and reduce cost [34]. Although a few types of complicated molecules were

Latent ruthenium–indenylidene catalysts bearing a N-heterocyclic carbene and a bidentate picolinate ligand

• Thibault E. Schmid,
• Florian Modicom,
• Adrien Dumas,
• Etienne Borré,
• Loic Toupet,
• Olivier Baslé and
• Marc Mauduit

Beilstein J. Org. Chem. 2015, 11, 1541–1546, doi:10.3762/bjoc.11.169

• improve the synthesis efficiency of the desired complex 4a, the [(SIPr)RuCl2(indenylidene)pyridine] complex 5 was used as a precursor (Scheme 2). The latter species offers both the advantages to avoid the use of phosphine scavenger and to trap the acid formed as a pyridinium chloride salt. Gratifyingly

Synthesis of a bifunctional cytidine derivative and its conjugation to RNA for in vitro selection of a cytidine deaminase ribozyme

• Nico Rublack and
• Sabine Müller

Beilstein J. Org. Chem. 2014, 10, 1906–1913, doi:10.3762/bjoc.10.198

• . In terms of synthesis efficiency, we first tried to simultaneously deprotect the amino functionality at the nucleobase and the sugar 5'-hydroxy group to generate derivative 12. Thereafter, the greater nucleophilicity of the primary amine over the alcohol should be used for selective amide bond