Patent ID: 7592392

Claim:
A process for the preparation of a compound of the formula I: wherein is an insoluble solid support selected from the group consisting of: poly(styrene-divinylbenzene), macroreticular poly(styrene-divinylbenzene), polystyrene which is radiation grafted to polypropylene, polystyrene which is radiation grafted to polyethylene, polystyrene which is radiation grafted to poly(tetrafluoroethylene), and polystyrene which is radiation grafted to poly(ethylene-tetrafluoroethylene) wherein the insoluble solid support is in a shape selected from a bead, a tube, a rod, a ring, a disk, or a well; L is —CH 2 —, —C(CH 3 ) 2 —, —CH(CH 3 )—, —(CH 2 ) n CH(CN)—, —(CH 2 ) n CH(CO 2 Me)-, —(CH 2 ) n CH(Ph)-, —(CH 2 ) n C(CH 3 , Ph)-, —CH(CH 2 CH 2 Ph)-, or n is zero or an integer from 1 to 5; m is zero or an integer from 1 to 100; b is mMol content of initiator or solid-supported polymer per gram of insoluble solid support and is about 0.1 to about 5.0 in mMol per gram; R 1 is selected from: wherein X is H, F, (CH 2 ) n Cl, (CH 2 ) n Br, (CH 2 ) n I, B(OH) 2 , (CH 2 ) n CH═CH 2 , NCO, CH 2 NCO, CH(CH 3 )NCO, C(CH 3 ) 2 NCO, CO 2 Me, CO 2 Et, CO 2 (t-Bu), CO 2 H, COCl, CO 2 CH(CF 3 ) 2 , CO 2 Ph, CO 2 (pentafluorophenyl), CO 2 (pentachlorophenyl), CO 2 (N-succinimidyl), C(OMe) 3 , C(OEt) 3 , (CH 2 ) n OH, (CH 2 ) n CH(OH)CH 2 0H, (CH 2 ) n SH, CH 2 NHCH 2 CH 2 SH, (CH 2 ) n NHC(═S)NH 2 , (CH 2 ) n NH 2 , (CH 2 ) n N(Me) 2 , (CH 2 ) n N(Et) 2 , (CH 2 ) n (iPr) 2 , CH(CH 3 )NH 2 , C(CH 3 ) 2 NH 2 , CH 2 NHCH 2 CH 2 NH 2 , CH 2 NHCH 2 CH 2 NHCH 2 CH 2 NH 2 , CH 2 N(CH 2 CH 2 NH 2 ) 2 , CH 2 NHCH 2 CH 2 N(CH 2 CH 2 NH 2 ) 2 , CH 2 N(CH 2 CH 2 0H) 2 , (CH 2 ) n (morpholin-4-yl), (CH 2 ) n (piperidin-1-yl), (CH 2 ) n (4-methypiperazin-1-yl), N(SO 2 CF 3 ) 2 , (CH 2 ) n CHO, (CH 2 ) n Si(Me) 2 H, (CH 2 ) n Si(Et) 2 H, (CH 2 )Si(iPr) 2 H, (CH 2 ) n Si(tBu) 2 H, (CH 2 ) n Si(Ph) 2 H, (CH 2 ) n Si(Ph)(tBu)H, (CH 2 ) n Si(Me) 2 Cl, (CH 2 ) n Si(Et) 2 Cl, (CH 2 ) n Si(i-Pr) 2 Cl, (CH 2 ) n Si(tBu) 2 Cl, (CH 2 ) n Si(Ph) 2 Cl, (CH 2 ) n Si(tBu)(Ph)Cl, P(Ph) 2 , P(o-tolyl) 2 , wherein n is zero or an integer from 1 to 5 Y is H, Cl, Br, F, OH, or OMe; Z is NCO, CO 2 Me, CO 2 Et, CO 2 (i-Pr), CO 2 (n-Bu), CO 2 (t-Bu), CN, CO 2 H, COCl, CO 2 CH(CF 3 ) 2 , C0 2 (pentafluorophenyl), CO 2 (pentachlorophenyl), CO 2 Ph, CO 2 (N-succinimidyl), C(OMe) 3 , C(OEt) 2 , CON(OCH 3 )CH 3 , CHO, CH 2 OH, or C(CH 3 ) 2 OH; and R 4 is which comprises the step of microwave irradiating a mixture comprising a compound of the formula II and a compound III selected from: