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    • 7. 发明申请
    • AN IMPROVED PROCESS FOR PREPARING TELMISARTAN
    • 改进TELMISARTAN的改进方法
    • WO2011102645A3
    • 2012-01-19
    • PCT/KR2011001041
    • 2011-02-17
    • DONG WHA PHARM CO LTDOH YOON-SEOKLIM JAE-KYUNGCHOI JUNG-UKKWON O-JINLEE JUN-SANG
    • OH YOON-SEOKLIM JAE-KYUNGCHOI JUNG-UKKWON O-JINLEE JUN-SANG
    • C07D403/10C07D403/04C07D403/06
    • C07D403/04
    • The present invention relates to an improved process for preparing telmisartan from 4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole and 2-[4-(bromomethyl)phenyl] benzoate by using condensation reaction and hydrolysis reaction wherein the condensation reaction is performed to prepare an intermediate by using mixed solvent of dimethyl sulfoxide and isopropanol as reaction solvent using dimethyl sulfoxide of 0.5~1.5 times and isopropanol of 1.5~4.5 times on the basis of the usage of 4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-prophyl-1H-benzimidazole and the hydrolysis reaction is performed to cause the reaction in mixed solvent of methanol of 7~9 times and purified water of 5~7 times on the basis of the intermediate. The process for preparing telmisartan according to the present invention provides a simple preparing process for mass production and improves a manufacturing yield with high purity by eliminating an additional process for removing an inorganic salt as a byproduct due to a base used in the condensation reaction and the hydrolysis reaction.
    • 本发明涉及从4-甲基-6-(1-甲基-1H-苯并咪唑-2-基)-2-丙基-1H-苯并咪唑和2- [4-(溴甲基)苯基]苯并咪唑制备替米沙坦的改进方法, 苯甲酸酯通过使用缩合反应和水解反应,其中通过使用二甲基亚砜和异丙醇的混合溶剂作为反应溶剂进行缩合反应,使用0.5〜1.5倍的二甲基亚砜和1.5〜4.5倍的异丙醇,基于 使用4-甲基-6-(1-甲基-1H-苯并咪唑-2-基)-2-预防-1H-苯并咪唑并进行水解反应,使甲醇混合溶剂中的反应为7〜9次, 纯化水为中间体5〜7次。 根据本发明的替米沙坦制备方法提供了一种简单的批量制备方法,通过除去由于缩合反应中使用的碱作为副产物而除去无机盐的附加方法,提高了高纯度的制造产率, 水解反应。
    • 9. 发明申请
    • AN IMPROVED PROCESS FOR PREPARING TELMISARTAN
    • 改进TELMISARTAN的改进方法
    • WO2011102645A2
    • 2011-08-25
    • PCT/KR2011/001041
    • 2011-02-17
    • DONG WHA PHARM. CO., LTD.OH, Yoon-SeokLIM, Jae-KyungCHOI, Jung-UkKWON, O-JinLEE, Jun-Sang
    • OH, Yoon-SeokLIM, Jae-KyungCHOI, Jung-UkKWON, O-JinLEE, Jun-Sang
    • C07D403/10C07D403/04C07D403/06
    • C07D403/04
    • The present invention relates to an improved process for preparing telmisartan from 4-methyl-6-(1-methyl-1 H -benzimidazole-2-yl)-2-propyl-1 H -benzimidazole and 2-[4-(bromomethyl)phenyl] benzoate by using condensation reaction and hydrolysis reaction wherein the condensation reaction is performed to prepare an intermediate by using mixed solvent of dimethyl sulfoxide and isopropanol as reaction solvent using dimethyl sulfoxide of 0.5~1.5 times and isopropanol of 1.5~4.5 times on the basis of the usage of 4-methyl-6-(1-methyl-1 H -benzimidazole-2-yl)-2-prophyl-1 H -benzimidazole and the hydrolysis reaction is performed to cause the reaction in mixed solvent of methanol of 7~9 times and purified water of 5~7 times on the basis of the intermediate. The process for preparing telmisartan according to the present invention provides a simple preparing process for mass production and improves a manufacturing yield with high purity by eliminating an additional process for removing an inorganic salt as a byproduct due to a base used in the condensation reaction and the hydrolysis reaction.
    • 本发明涉及从4-甲基-6-(1-甲基-1H-苯并咪唑-2-基)-2-丙基-1H-苯并咪唑和2- [4-(溴甲基)苯基]苯并咪唑制备替米沙坦的改进方法, 苯甲酸酯通过使用缩合反应和水解反应,其中通过使用二甲基亚砜和异丙醇的混合溶剂作为反应溶剂进行缩合反应,使用0.5〜1.5倍的二甲基亚砜和1.5〜4.5倍的异丙醇,基于 使用4-甲基-6-(1-甲基-1H-苯并咪唑-2-基)-2-预防-1H-苯并咪唑并进行水解反应,使甲醇混合溶剂中的反应为7〜9次, 纯化水为中间体5〜7次。 根据本发明的替米沙坦制备方法提供了一种简单的批量制备方法,通过除去由于缩合反应中使用的碱作为副产物而除去无机盐的附加方法,提高了高纯度的制造产率, 水解反应。
    • 10. 发明申请
    • METHOD FOR PREPARING ADHESIVE ACRYLIC ESTER POLYMER SYRUP
    • 制备丙烯酸酯聚合物SYRUP的方法
    • WO2006129974A1
    • 2006-12-07
    • PCT/KR2006/002104
    • 2006-06-01
    • LG CHEM, LTD.PARK, Jong-suhCHOI, Sun-HyukCHOI, Jung-uk
    • PARK, Jong-suhCHOI, Sun-HyukCHOI, Jung-uk
    • C08F2/02
    • C09J133/06C08F2/02
    • The present invention relates to a method for preparing an acrylic ester polymer syrup by bulk polymerization, and more particularly, to a method for preparing an acrylic ester polymer syrup, which comprises the steps of: supplying a monomer solution and an initiator solution to a monomer solution reservoir and an initiator solution reservoir, respectively; supplying the monomer solution and the initiator solution to a complete-mixing type continuous reactor, while maintaining the dissolved oxygen in the monomer solution reservoir and the initiator solution reservoir at 0.0001 to 3 ppm, separately or after mixing prior to the supply; and performing bulk polymerization continuously while maintaining the solution mixture supplied to the continuous reactor at 70 to 150 0C and 1 to 10 atm, with a mean residence time of 30 to 240 minutes. In accordance with the present invention, an acrylic ester polymer syrup can be obtained with a degree of polymerization of 20 to 70 % at a low polymerization temperature, even with a small amount of initiator. Productivity can be improved by reducing reaction time with the use of an initiator having a short half-life and polymerization can be performed very stably and continuously without gelation.
    • 本发明涉及通过本体聚合制备丙烯酸酯聚合物浆料的方法,更具体地说,涉及一种制备丙烯酸酯聚合物浆料的方法,其包括以下步骤:向单体供应单体溶液和引发剂溶液 溶液储层和引发剂溶液储层; 将单体溶液和引发剂溶液供应到完全混合型连续反应器,同时将单体溶液储存器和引发剂溶液储存器中的溶解氧分别维持在0.0001至3ppm,或在供给之前混合; 并连续进行本体聚合,同时将提供给连续反应器的溶液混合物保持在70〜150℃和1〜10atm,平均停留时间为30〜240分钟。 根据本发明,即使使用少量的引发剂,也可以在低聚合温度下聚合度为20〜70%的丙烯酸酯聚合物糖浆。 通过使用半衰期短的引发剂减少反应时间可以提高生产率,聚合可以非常稳定和连续地进行而没有凝胶化。