6-氟-3-哌啶-4-基-1,2-苯并异唑盐酸盐合成路线 （共 28 条）
反应条件
1: 1-bromo-3-chloro-propane; 4'-hydroxy-3'-methoxyacetophenone With tetrabutylammomium bromide; potassium carbonate in acetonitrile T=80°C; Industry scale; 2: 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole monohydrochloride With tetrabutylammomium bromide; potassium carbonate in methanol T=60 - 65°C; autoclave;
参考文献
LUPIN LIMITED; ANSARI, Shahid, Akhtar; HIRPARA, Hitin, Maganbhai; YADAV, Ashok, Keshavlal; GIANCHANDANI, Jaya, Parasram
Patent: WO2012/164516 A1, 2012 ;
Location in patent: Page/Page column 4-5 ;
反应条件
1: 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole monohydrochloride With sodium hydroxide in water T=25 - 30°C; 0.25 h; Industrial scaleGreen chemistry; 2: 1-[4-(3-chloropropoxy)-3-methoxyphenyl]ethanone in water T=25 - 30°C; 0.25 h; Industrial scaleGreen chemistry; 3: With tetrabutylammomium bromide in n-heptane; water T=65 - 70°C; Industrial scaleGreen chemistry; Reagent/catalystSolventTemperatureConcentrationTime;
参考文献
Solanki, Pavankumar V.; Uppelli, Sekhar Babu; Pandit, Bhushan S.; Mathad, Vijayavitthal T.
Organic Process Research and Development, 2014 , vol. 18, # 2 p. 342 - 348
反应条件
in N-methyl-acetamide
参考文献
Hoechst-Roussel Pharmaceuticals, Inc.
Patent: US5364866 A1, 1994 ;
反应条件
1.1: potassium carbonate / acetonitrile / 60 - 85 °C 1.2: 0 - 30 °C 2.1: triethylamine / methanol View Scheme
参考文献
ORCHID CHEMICALS AND PHARMACEUTICALS LIMITED; REGURI, Buchi, Reddy; ARUNAGIRI, Muthulingam; YARROJU, Prasada, Chari; KASIYAPPAN GURUSAMY, Saravanakumar; PONNAPALLI, Kondalarao
Patent: WO2011/55188 A1, 2011 ;
反应条件
in N,N-dimethyl-formamide
参考文献
Organic Process Research and Development, , vol. 18, # 2 p. 342 - 348
反应条件
N-ethyl-N,N-diisopropylamine in methanol 24 h; Reflux;
参考文献
Laboratorios Lesvi, S.L.
Patent: EP2202234 A1, 2010 ;
Location in patent: Page/Page column 7 ;
反应条件
1: 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole monohydrochloride With potassium carbonate; potassium iodide in acetonitrile T=30 - 60°C; 2: (±)-3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride in acetonitrile T=60°C; 47 h;
参考文献
CADILA PHARMACEUTICALS LTD.; MODI, Indravadan, Ambalal; SODAGAR, Keval, Rameshchandra; VINEET, Malik; JAIN, Sudhir, Hukamchand; PARIKH, Sanjay, Natvarlal; SHARMA, Arun, Omprakash; BAPAT, Uday, Rajaram; KHAMAR, Bakulesh, Mafatlal
Patent: WO2010/64134 A2, 2010 ;
Location in patent: Page/Page column 7 ;
反应条件
ammonia in methanol; chloroform
参考文献
Janssen Pharmaceutica N.V.
Patent: US5158952 A1, 1992 ;
US 5158952 A
反应条件
in methanol; water; acetone
参考文献
Padi, Pratap Reddy; Bollikonda, Satyanarayana; Akundi, Surya Prabhakar; Cherukupally, Praveen; Suthrapu, Sashikanth; Mohanarangam, Saravanan; Kandirelli, Venkat Kiran; Chellu, Malleswara Rao; Pagadala, Narasimha Rao
Patent: US2009/48272 A1, 2009 ;
反应条件
in methanol; water; acetone
参考文献
Padi, Pratap Reddy; Bollikonda, Satyanarayana; Akundi, Surya Prabhakar; Cherukupally, Praveen; Suthrapu, Sashikanth; Mohanarangam, Saravanan; Kandirelli, Venkat Kiran; Chellu, Malleswara Rao; Pagadala, Narasimha Rao
Patent: US2009/48272 A1, 2009 ;
