87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.
EXAMPLE 59; (R)(-)-N-{5-[2-(4-BENZO[D]ISOTHIAZOL-3-YL-PIPERAZIN-1-YL)- ETHYL1-INDAN-2-YLl-ACETAMIDE; A slurry of (R)-N- [5- (2-Chloro-ethyl)-indan-2-yl]-acetamide (2. 00g, 8. 41mmole), Na2CO3(1. 5eq) and 3-Piperazin-1-yl-benzo [d] isothiazole hydrochloride (2. 0eq) in H20 (20moi) was reacted under microwave assistance using a CEM MARS-5 microwave reactor to 175C for 10min. Upon cooling, the reaction was diluted with EtOAc (250moi), H20 (100mol) and the layers separated. The aqueous layer was extracted with EtOAc (2x 50ml). The organics were dried (MgSO4), concentrated, and the residue purified by chromatography (EtOAc) to give (R) (-)-N- {5- [2- (4- Benzo [d] isothiazol-3-yl-piperazin-1-yl)-ethyl]-indan-2-yl}-acetamide (2. 92g, 6. 94mmole) in 100% purity 254 nm; LCMS (APCI) 474 [M+H] +. [a] D25- 3. 6 (c 5.5, CHCl3). 1 H NMR (400 MHz, CHLOROFORM-D) 8 ppm 1.94 (s, 3 H) 2.65-2. 71 (m, 2 H) 2.73-2. 80 (m, 6 H) 2.81-2. 87 (m, 2 H) 3.28 (ddd, J=16. 04,6. 10,5. 92 Hz, 2 H) 3.57-3. 62 (m, 4 H) 4.69-4. 76 (m, 1 H) 5.70 (d, J=7.08 Hz, 1 H) 7.06 (d, J=7.81 Hz, 1 H) 7.11 (s, 1 H) 7.16 (d, J=7.56 Hz, 1 H) 7.35 (ddd, J=8.17, 7.08, 1.10 Hz, 1 H) 7.46 (ddd, J=8.11, 7.02, 1.22 Hz, 1 H) 7.81 (dt, J=8.05, 0.85 Hz, 1 H) 7.91 (dt, J=8.30, 0.98 Hz, 1 H).
The chemical industry reduces the impact on the environment during synthesis,87691-88-1,3-Piperazinobenzisothiazole hydrochloride,I believe this compound will play a more active role in future production and life.
Reference£º
Patent; WARNER-LAMBERT COMPANY LLC?; WO2005/56540; (2005); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com