Recent developments in chemical diversity

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Editor: John A. Porco Jr.
Boston University
 
Diversity-oriented synthesis (DOS) is an important field involving the synthesis of libraries of diverse small molecules for applications including biological screening. The last decade has witnessed major progress in the field, with continued emphasis on structural and functional diversity for DOS library construction, leading to recent successes of biologically active molecules obtained from DOS compound collections. In the original paradigm for DOS, compound and library design were often based on the incorporation of functional, skeletal, and stereochemical diversity elements. An emerging theme in the area involves the development of novel reaction methodologies as a means to access or discover new “chemotypes”, advancing alongside the technology that enables progress in this area. In this way, organic chemists are empowered by the paradigm of “chemical diversity as a function of novel chemical reactions”, exploring a diverse repertoire of approaches to achieve their goals.
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Recent developments in chemical diversity

  • John A. Porco Jr

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

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Published 06 Jun 2012

An intramolecular inverse electron demand Diels–Alder approach to annulated α-carbolines

  • Zhiyuan Ma,
  • Feng Ni,
  • Grace H. C. Woo,
  • Sie-Mun Lo,
  • Philip M. Roveto,
  • Scott E. Schaus and
  • John K. Snyder

Beilstein J. Org. Chem. 2012, 8, 829–840, doi:10.3762/bjoc.8.93

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Published 06 Jun 2012

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

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Published 06 Jun 2012

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

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Published 06 Jun 2012

Parallel and four-step synthesis of natural-product-inspired scaffolds through modular assembly and divergent cyclization

  • Hiroki Oguri,
  • Haruki Mizoguchi,
  • Hideaki Oikawa,
  • Aki Ishiyama,
  • Masato Iwatsuki,
  • Kazuhiko Otoguro and
  • Satoshi Ōmura

Beilstein J. Org. Chem. 2012, 8, 930–940, doi:10.3762/bjoc.8.105

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Published 22 Jun 2012

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

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Letter
Published 02 Jul 2012

Parallel solid-phase synthesis of diaryltriazoles

  • Matthias Wrobel,
  • Jeffrey Aubé and
  • Burkhard König

Beilstein J. Org. Chem. 2012, 8, 1027–1036, doi:10.3762/bjoc.8.115

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Published 06 Jul 2012

Synthesis and in silico screening of a library of β-carboline-containing compounds

  • Kay M. Brummond,
  • John R. Goodell,
  • Matthew G. LaPorte,
  • Lirong Wang and
  • Xiang-Qun Xie

Beilstein J. Org. Chem. 2012, 8, 1048–1058, doi:10.3762/bjoc.8.117

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Published 10 Jul 2012

Synthesis of a library of tricyclic azepinoisoindolinones

  • Bettina Miller,
  • Shuli Mao,
  • Kara M. George Rosenker,
  • Joshua G. Pierce and
  • Peter Wipf

Beilstein J. Org. Chem. 2012, 8, 1091–1097, doi:10.3762/bjoc.8.120

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Published 13 Jul 2012

Synthesis of diverse indole libraries on polystyrene resin – Scope and limitations of an organometallic reaction on solid supports

  • Kerstin Knepper,
  • Sylvia Vanderheiden and
  • Stefan Bräse

Beilstein J. Org. Chem. 2012, 8, 1191–1199, doi:10.3762/bjoc.8.132

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Published 26 Jul 2012

Palladium-catalyzed substitution of (coumarinyl)methyl acetates with C-, N-, and S-nucleophiles

  • Kalicharan Chattopadhyay,
  • Erik Fenster,
  • Alexander J. Grenning and
  • Jon A. Tunge

Beilstein J. Org. Chem. 2012, 8, 1200–1207, doi:10.3762/bjoc.8.133

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Published 27 Jul 2012

Photochemistry with laser radiation in condensed phase using miniaturized photoreactors

  • Elke Bremus-Köbberling,
  • Arnold Gillner,
  • Frank Avemaria,
  • Céline Réthoré and
  • Stefan Bräse

Beilstein J. Org. Chem. 2012, 8, 1213–1218, doi:10.3762/bjoc.8.135

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Published 31 Jul 2012

Exploring chemical diversity via a modular reaction pairing strategy

  • Joanna K. Loh,
  • Sun Young Yoon,
  • Thiwanka B. Samarakoon,
  • Alan Rolfe,
  • Patrick Porubsky,
  • Benjamin Neuenswander,
  • Gerald H. Lushington and
  • Paul R. Hanson

Beilstein J. Org. Chem. 2012, 8, 1293–1302, doi:10.3762/bjoc.8.147

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Published 15 Aug 2012

Synthesis of a novel chemotype via sequential metal-catalyzed cycloisomerizations

  • Bo Leng,
  • Stephanie Chichetti,
  • Shun Su,
  • Aaron B. Beeler and
  • John A. Porco Jr.

Beilstein J. Org. Chem. 2012, 8, 1338–1343, doi:10.3762/bjoc.8.153

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Published 20 Aug 2012

Automated three-component synthesis of a library of γ-lactams

  • Erik Fenster,
  • David Hill,
  • Oliver Reiser and
  • Jeffrey Aubé

Beilstein J. Org. Chem. 2012, 8, 1804–1813, doi:10.3762/bjoc.8.206

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Published 19 Oct 2012
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