Downstream synthetic route of 129779-30-2

As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

148 6-((3R.5SV3.5-Dimethyl-4-thiazol-2-ylmethyl-rhoirhoerazin-l-ylmethvn-2-(lH- indazol-4-yl)-4-morpholin-4- yl-thieno [3.2-d]p yrimidine.Via 2-chloro-6-((3R,5 S)-3 ,5 -dimethyl-4-thiazol-2-ylmethyl-piperazin- 1 – ylmethyl)-4-mophiholin-4-yl-thieno[3,2-d]pyrimidine, prepared from (2R,6S)-2,6- dimethyl- 1 -thiazol-2-ylmethyl-piperazine.Amine preparation: 2-Thiazolecarboxaldehyde was converted to the corresponding alcohol by treatment with sodium borohydride. Reaction with methanesulfonyl chloride yielded methanesulfonic acid thiazol-2-ylmethyl ester. A mixture of methanesulfonic acid thiazol-2-ylmethyl ester (393mg), (3R,5S)-3,5- dimethyl-piperazine-1 -carboxylic acid tert-butyl ester (described previously, 435mg), potassium carbonate (309mg) and tetrabutyl ammonium iodide (827mg) was heated to reflux in MeCN (1OmL). After 4 days the reaction mixture was cooled, diluted with ethyl acetate, washed with water and dried (MgSO4). The solvent was evaporated and the residue purified by flash chromatography to give (R)-3,5- dimethyl-4-thiazol-2-ylmethyl-piperazine-l -carboxylic acid (S) -tert-butyl ester (314mg). Treatment of this compound with HCl in DCM/MeOH yielded the desired amine, which was isolated as the hydrochloride salt. EPO 1H NMR (400MHz, CDCl3) 1.12 (d, J=6.0Hz, 6H), 2.06 (m, 2H), 2.85 (m, 4H), 3.80 (s, 2H), 3.92 (m, 4H), 4.09 (m, 4H), 4.17 (s, 2H), 7.24 (d, J=3.2Hz, IH), 7.38 (s, IH), 7.51 (m, IH), 7.59 (d, J=8.3Hz, IH), 7.74 (d, J=3.3Hz, IH), 8.29 (d, J=7.3Hz, IH), 9.03 (s, IH), 10.1 (br s, IH); MS (ESf) 561 (MH+)., 129779-30-2

As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference£º
Patent; PIRAMED LIMITED; WO2006/46031; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics