Pinchuk, Anatoly et al. published their patent in 2008 |CAS: 78-26-2

The Article related to phospholipid ether boronic acid ester analog preparation cancer treatment, radiation therapy phospholipid ether boronic acid ester radiohalogenated analog, alkyl phosphocholine boronic acid ester analog preparation cancer treatment and other aspects.Recommanded Product: 2-Methyl-2-propylpropane-1,3-diol

On December 11, 2008, Pinchuk, Anatoly; Weichert, Jamey P.; Longino, Marc published a patent.Recommanded Product: 2-Methyl-2-propylpropane-1,3-diol The title of the patent was Methods for the synthesis and use of phospholipid ether boronic acids and esters. And the patent contained the following:

The present invention discloses boronic acids and esters I [A = (CH2)n; X = boronic acid or ester; Y = NH2, NHR, NR2, NR+3; R = alkyl, arylalkly; n = 8 – 30], II [M = Li, Na, K, Cs, Rb] and III [Z = H, OH, OMe, OEt, OPr], of phospholipid ether (PLE) analogs and methods for their synthesis and use. A method of synthesizing a high specific activity PLE analog comprises: (a) coupling of a diboron with a PLE or alkyl phosphocholine (APC) analog in the presence of a catalyst to result in a boronic acid or ester PLE or APC analog; (b) optionally esterification the boronic acid of the PLE analog with 1,2- or 1,3-diols to result in the boronic esters of PLE or APC analogs; and, (c) optionally, reacting the boronic acid of ester of PLE or APC analog of (a) or (b) with sodium radiohalide, in the presence of an oxidant to result in a high specific activity radiohalogenated PLE or APC analog. Thus, NM404 (IV) was prepared from 4-IC6H4CH2Br via coupling with BrZn(CH2)11OAc, deacetylation with NaOH, Iodination with I2/PPH3/imidazole, coupling with BrZn(CH2)5CO2Et, saponification with NaOH, reduction with BH3·THF, phosphorylation with ethylene chlorophosphate, and reaction with NMe3. Coupling reaction of IV with bis(neopentylglycolato)diboron in MeOH containing KOAc and catalytic PdCl2(DPPF) gave II [X = B(OH)2], while coupling with bis(pinacolato)diboron gave II [X = pinacolborane]. Reaction of II [X = B(OH)2] with Na125I in aqueous NaOH containing chloramine-T gave 125I-NM404. The boronic acids and esters of phospholipid ether analogs described herein can be used in treating cancer and in particular can be used in conjunction with radiation therapy, such as external beam radiation therapy and neutron capture therapy to specifically target and kill cancer cells [see graphs]. The experimental process involved the reaction of 2-Methyl-2-propylpropane-1,3-diol(cas: 78-26-2).Recommanded Product: 2-Methyl-2-propylpropane-1,3-diol

The Article related to phospholipid ether boronic acid ester analog preparation cancer treatment, radiation therapy phospholipid ether boronic acid ester radiohalogenated analog, alkyl phosphocholine boronic acid ester analog preparation cancer treatment and other aspects.Recommanded Product: 2-Methyl-2-propylpropane-1,3-diol

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