Solid Phase Synthesis

Functionalized Ionic Liquids as New Supports for Peptide Coupling and Traceless Catalyzed Carbon-Carbon Coupling Reactions

“…For instance, insoluble polymeric supports were designed to facilitate product purification through simple filtration and rinsing. Although successful, solid phase synthesis (SPS) has several shortcomings that arise by the nature of the heterogeneous reaction conditions [2,3]. To overcome these limitations, liquid-phase combinatorial synthesis (LPCS), involving soluble polymers and fluorous systems, has been developed as an alternative methodology [4][5][6][7][8].…”

A Simple, Rapid and Mild One Pot Synthesis of Benzene Ring Acylated and Demethylated Analogues of Harmine under Solvent-free Conditions

“…Further workup using column chromatography (silica gel; Merck 9385; CHCl 3 -MeOH, in increasing order of polarity from 9.95:0.05 to 9.5:0.5) afforded 10,12-diacyl,11-hydroxy (23-30; TLC data: R f ~ 0.90, 9.5:0.5 CHCl 3 -MeOH), 12-acyl (10-17; TLC data: R f ~ 0.86, 9.5:0.5 CHCl 3 -MeOH), 10-acyl,11-hydroxy (18-22; TLC data: R f ~ 0.70, 9.5:0.5 CHCl 3 -MeOH ) and 10-acyl (2-9; TLC data: R f ~ 0.61, 9.5:0.5 CHCl 3 -MeOH) derivatives, respectively, as colorless crystalline solids, in moderate yields (Table 1). (2 (8 (12 (14 (16 (18 Note: NMRs of 3 and 18 were recorded in CD 3 OD, whereas those of 11 and 24 were recorded in CDCl 3 . Assignments were established by interpretation of the 13 C-NMR (broad band decoupled and DEPT), HMQC, and HMBC spectra.…”

“…An additional attractive feature is their operational simplicity. Thus, there are now over 500 published papers describing solvent-free reactions giving quantitative yields on the gram and kilogram scale that support the effectiveness of the method [1][2][3][4].…”

Recent Advances in the Solid-Phase Combinatorial Synthetic Strategies for the Quinoxaline, Quinazoline and Benzimidazole Based Privileged Structures

“…Houghten and co-workers recently reported [140] a solid-phase synthesis of substituted [1,3,5]triazino[1,2-a]benzimadazole-2,4(3H,10H)-diones. The synthetic strategy starts from resinbound amines.…”

“…The advances recently made in solid-phase organic synthesis (SPOS) have led to the success of combinatorial chemistry [3]. This has given an opportunity of preparing compounds by new routes [4], which is usually not that easy by employing conventional solution-phase procedures and eventually saving time for purification [5]. Therefore, generation of small molecule libraries derived from heterocyclic structures can be executed effectively by employing combinatorial or simultaneous parallel synthesis on solid-support [6][7][8][9][10].…”