By Willi Bannwarth, Eduard Felder, Raimund Mannhold, Hugo Kubinyi, Hendrik Timmerman

As we input the recent millennium, combinatorial chemistry is offering major impetus to new options in man made chemistry. Combinatorial chemistry has swiftly develop into the emerging megastar between study tools, permitting scientists to successfully try the feasibility of a mess of latest compounds. The pursuit of latest medicines is yet one difficult box during which those combinatorial tools are rather helpful, supporting researchers meet the modern day calls for of a hugely aggressive setting. This ebook emphasises that glossy combinatorial synthesis is feasible not just within the good part, but in addition in ideas. furthermore, it discusses computer-assisted equipment in addition to the gear and instrumentation required for the combinatorial technique. winning and skilled researchers within the best pharmaceutical businesses and most famed study institutes provide an excellent perception and point of view into this various box. A 'must' for each scientist within the region of pharmaceutical learn.

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Additional resources for Combinatorial Chemistry: A Practical Approach (Methods and Principles in Medicinal Chemistry)

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59,3631-3635 (1986). , Tetrahedron Lett. 39,5869-5872 (1998). , J. Org. Chem. 63,6234-6238 (1998). , Tetrahedron Lett. 38,63474350 (1997). , Tetrahedron Lett. 39,967-970 (1998). , Tetrahedron Lett. 39, 44494452 (1998). , Tetrahedron Lett. 39,3647-3650 (1998). , J. Am. Chem. 107,1768-1769 (1985). , Comprehensive Organic Synthesis, Vol. , Fleming I. ). Pergamon, Oxford. , Synthesis 1195-1202 (1995). , Armstrong R. , Tetrahedron Lett. 38,61634166 (1997). 1, the benefits of solution-phase synthesis over solid-phase synthesis are the following.

Heteroaromatic amidines 13 react with an isonitrile and an aldehyde in the presence of catalytic amounts of a protic acid. The reaction proceeds with high efficiency to yield 3-amino-imidazo [1,2-a] pyri(mi)dines of the general type 14. R’CHO T N ] o R 2 + R3NC H+ MeOH 13 H NHR3 14 b Scheme 8 The reaction proceeded well in methanol and was not sensitive to moisture or oxygen. With respect to the reactivity of aldehydes there was virtually no limitation. , adenine) did not react. With regard to the reaction mechanism, the authors assumed a nonconcerted [4+1]-cycloaddition, as outlined in Scheme 8.

63,3454-3457 (1998). , Tetrahedron Lett. 36,7819-7822 (1995). , Med. Res. Rev. 9,291-324 (1989). 5114516 (1995). , Tetrahedron Lett. 39,1117-1120 (1998). , Heterocycl. Commun. 2, 359-360 (1996). , Tetrahedron Lett. 39,2235-2238 (1998). , Bull. Chem. Jpn. 59,3631-3635 (1986). , Tetrahedron Lett. 39,5869-5872 (1998). , J. Org. Chem. 63,6234-6238 (1998). , Tetrahedron Lett. 38,63474350 (1997). , Tetrahedron Lett. 39,967-970 (1998). , Tetrahedron Lett. 39, 44494452 (1998). , Tetrahedron Lett. 39,3647-3650 (1998).

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