CAS: 170151-24-3; 4-(Aminomethyl)-3-[(2S)-5,7-Difluoro-1,2,3,4-Tetrahydronaphthalen-2-Yl]-1H-Imidazole-2-Thione,Hydrochloride

1,3-二氟苯置于三氯化铝 盐酸,Lithium Hydroxide Monohydrate,五氯化磷,硫酸,Sodium Acetate Trihydrate体系中,用 甲醇,Sodium Hydroxide,(2S)-N-Methyl-1-Phenylpropan-2-Amine Hydrate,正己烷,正庚烷,二氯甲烷,氮,水,溶剂黄146,乙酸乙酯,异丙醇,甲苯,三氟乙酸 用作溶剂,化学反应生成内匹司他盐酸盐
参考文献:Process For Making 1-Benzocycloalkyl-1,3-Dihydroimidazole-2-Thione
标题:Process For Making 1-Benzocycloalkyl-1,3-Dihydroimidazole-2-Thione
摘要:本发明涉及一种制备5-(N-取代)氨甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫醚的方法(其中n取代基选择自甲酰基,氨基甲酰基,(c.Sub.1-4)烷基甲酰基或三氟(c.Sub.1-4)烷基甲酰基),该方法包括将苯并环烷基胺与硫氰酸和双羟乙酮反应,得到相应的5-羟甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫醚,然后将5-羟甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫醚与式为h.Sub.2 Nc(0)R.Sup.2(其中r.Sup.2为氢,氨基,(c.Sub.1-4)烷基或三氟(c.Sub.1-4)烷基)的化合物反应,或与式为nh.Sub.4.Sup.+-oc(0)R.Sup.3(其中r.Sup.3为氢,(c.Sub.1-4)烷基或三氟(c.Sub.1-4)烷基)的铵盐反应.本发明还涉及一种制备5-氨甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫醚的方法,该方法包括通过上述描述的方法制备5-(N-取代)氨甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫醚(其中n取代基选择自甲酰基,(c.Sub.1-4)烷基甲酰基或三氟(c.Sub.1-4)烷基甲酰基),然后用酸进行水解.

专利信息

专利号:US-2022267331-A1
优先权日:2019-06-05
标题 :Dopamine-b-hydroxylase inhibitors
发明人：KISS LASZLO; BELIAEV ALEXANDER; ROSSI TINO; PALMA NUNO; SOARES DA SILVA PATRÃ?CIO; PINTO RUI; CARDONA FRANCISCO
权利人:BIAL PORTELA & CA SA
摘要:This invention relates to: (a) compounds of formula I (with R1 to R5 and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:US-11434242-B2
优先权日:2017-12-04
标题:Dopamine-b-hydroxylase inhibitors
发明人：KISS LASZLO ERNO; BELIAEV ALEXANDER; ROSSI TINO; PALMA PEDRO NUNO LEAL; SOARES DA SILVA PATRÃ?CIO MANUEL VIEIRA ARAUJO; PINTO RUI; CARDONA FRANCISCO
权利人:BIAL PORTELA & Cª S A; BIAL—PORTELA & CA S A
摘要:This invention relates to: (a) compounds of formula Ia (with R1, R4 to R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions (comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:CN-111018663-A
优先权日:2019-12-02
标 题 :A kind of important intermediate of nepicastat and method for its enzyme-catalyzed synthesis