Synthesis of (−)-julocrotine and a diversity oriented Ugi-approach to analogues and probes

• Ricardo A. W. Neves Filho,
• Bernhard Westermann and
• Ludger A. Wessjohann

Beilstein J. Org. Chem. 2011, 7, 1504–1507, doi:10.3762/bjoc.7.175

• ]. In addition, the glutarimide motif can be considered as a privileged structure. Compounds with this pharmacophore often exhibit a wide range of biological properties including anti-inflammatory [10], antitumor [11][12], and anticonvulsive properties [13]. Because of the low yields of julocrotine

Manganese dioxide mediated one-pot synthesis of methyl 9H-pyrido[3,4-b]indole-1-carboxylate: Concise synthesis of alangiobussinine

• Jessica Baiget,
• Sabin Llona-Minguez,
• Stuart Lang,
• Simon P. MacKay,
• Colin J. Suckling and
• Oliver B. Sutcliffe

Beilstein J. Org. Chem. 2011, 7, 1407–1411, doi:10.3762/bjoc.7.164

• Strathclyde, 295 Cathedral Street, Glasgow, G1 1XL, UK 10.3762/bjoc.7.164 Abstract The carboline ring system is an important pharmacophore found in a number of biologically important targets. Development of synthetic routes for the preparation of these compounds is important in order to prepare a range of

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

• Marcus Baumann,
• Ian R. Baxendale,
• Steven V. Ley and
• Nikzad Nikbin

Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57

• diaminobenzoates was obtained (Scheme 42) [64]. Telmisartan (217, Micardis) is a well known angiotensin II receptor antagonist used in the treatment of hypertension and, heart and bladder diseases. Its pharmacophore consists of two linked benzimidazoles and a biphenyl unit (Scheme 43). As shown previously, such

Novel tetracyclic structures from the synthesis of thiolactone-isatin hybrids

• Renate Hazel Hans,
• Hong Su and
• Kelly Chibale

Beilstein J. Org. Chem. 2010, 6, No. 78, doi:10.3762/bjoc.6.78

• natural and natural product-like hybrid constructs such as the artemisinin-quinine [2], nostocarboline-ciprofloxacin [3] and isatin-lamuvidine [4] (Figure 1). Interest in exploring this approach also derives from the pharmacophore-rich compound library it offers. This precludes the need for large

Synthesis of spiroannulated and 3-arylated 1,2,4-trioxanes from mesitylol and methyl 4-hydroxytiglate by photooxygenation and peroxyacetalization

• Axel G. Griesbeck,
• Lars-Oliver Höinck and
• Jörg M. Neudörfl

Beilstein J. Org. Chem. 2010, 6, No. 61, doi:10.3762/bjoc.6.61

• might show promise in overcoming the forthcoming problem of artemisinin resistance [8]. From a synthetic point of view, the preparation of the pharmacophore, the central 1,2,4-trioxane ring system, is possible by a number of strategies [9][10]. We, for example, have previously reported the use of the

ADDP and PS-PPh₃: an efficient Mitsunobu protocol for the preparation of pyridine ether PPAR agonists

• Paul S. Humphries,
• Quyen-Quyen T. Do and
• David M. Wilhite

Beilstein J. Org. Chem. 2006, 2, No. 21, doi:10.1186/1860-5397-2-21

• -2,4-dione pharmacophore.[12] These were propanoic acid derivatives with α-substitution to collectively serve as a mimic for the thiazolidine-2,4-dione ring. Based on the above and a knowledge of PPAR ligands publicly disclosed, we wished to synthesize compounds represented by the general structure 1