Two-directional synthesis as a tool for diversity-oriented synthesis: Synthesis of alkaloid scaffolds

• Kieron M. G. O’Connell,
• Monica Díaz-Gavilán,
• Warren R. J. D. Galloway and
• David R. Spring

Beilstein J. Org. Chem. 2012, 8, 850–860, doi:10.3762/bjoc.8.95

• particular reference to the synthesis of polycyclic alkaloid scaffolds. Keywords: alkaloids; cascade reactions; chemical diversity; diversity-oriented synthesis; Lewis acid catalysis; two-directional synthesis; Introduction Diversity-oriented synthesis (DOS) aims to prepare structurally diverse compound

Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors

• Chao Che,
• Song Li,
• Bo Yang,
• Shengchang Xin,
• Zhixiong Yu,
• Taofeng Shao,
• Chuanye Tao,
• Shuo Lin and
• Zhen Yang

Beilstein J. Org. Chem. 2012, 8, 841–849, doi:10.3762/bjoc.8.94

• relationship of this important class of hedgehog-pathway inhibitors. Keywords: chemical diversity; diversity-oriented; hedgehog pathway; inhibitor; Sant-75; synthesis; Introduction The Hedgehog (Hh) signaling pathway plays an essential role in embryonic development and adult tissue homeostasis in metazoans

• cyclization with acetamidine to give 16. Compound 11g could be installed in single step by Ullmann coupling of 17 with 4-bromopyridine, in good yield. Substituent-modifications on the motif C In the third round of structural modifications, chemical diversity was explored by varying the nature of the

Recent developments in chemical diversity

• John A. Porco Jr

Beilstein J. Org. Chem. 2012, 8, 827–828, doi:10.3762/bjoc.8.92

• John A. Porco Jr Boston University, Department of Chemistry, 590 Commonwealth Avenue, Boston MA 02215, USA 10.3762/bjoc.8.92 Keywords: chemical diversity; Diversity-oriented synthesis (DOS) is an important field involving the synthesis of libraries of diverse small molecules for applications

• molecules obtained from DOS compound collections [1][2]. This Thematic Series of the Beilstein Journal of Organic Chemistry attempts to capture recent developments in the area of chemical diversity and highlights the development of chemical reaction methodologies, the construction of novel chemotypes, and

• participating contributions in the Thematic Series, involves the development of novel reaction methodologies as a means to access or discover new “chemotypes”. In this way, organic chemists are empowered by the paradigm of “chemical diversity as a function of novel chemical reactions”. “Recent developments in

Gold(I)-catalyzed synthesis of γ-vinylbutyrolactones by intramolecular oxaallylic alkylation with alcohols

• Michel Chiarucci,
• Mirko Locritani,
• Gianpiero Cera and
• Marco Bandini

Beilstein J. Org. Chem. 2011, 7, 1198–1204, doi:10.3762/bjoc.7.139

• activation of allylic alcohols [27][28][29][30][31] with esters [32][33][34][35][36][37]. In this direction, we targeted malonyl alcohols 1 as a readily available class of model acyclic precursors to create chemical diversity through an oxaallylic ring-closing reaction (Figure 1). It should be noted that the