发明名称 AN IMPROVED PROCESS FOR MAKING ZILPATEROL
摘要 This invention generally relates to processes for making zilpaterol and salts thereof, as well as processes for making intermediates that, interalia, may be used to make zilpaterol and salts thereof.
申请公布号 US2015315195(A1) 申请公布日期 2015.11.05
申请号 US201314652585 申请日期 2013.12.17
申请人 INTERVET INTERNATIONAL B.V. ;INTERVET INC. 发明人 Towson James C.;Wong Shing-Chun
分类号 C07D487/04 主分类号 C07D487/04
代理机构 代理人
主权项 1. A method of preparing a compound of Formula I or a salt thereofcomprising: a. reacting a compound of Formula IIwith a halogenating agent to produce a compound of Formula IIIwherein X is CI, Br, or I; b. reacting compound III with a compound of Formula Ato produce a compound of Formula IV;and c. reacting compound IV with a reducing agent to produce a compound of Formula I wherein: R1 is selected from hydrogen, amino, alkyl, alkenyl, alkynyl, aryl, benzyl, or any cyclic version or heteroatom containing version thereof and wherein for each alkyl, alkenyl, alkynyl, aryl, benzyl, and any cyclic version or heteroatom containing version may be substituted or unsubstituted; R2a and R2b are the same or different and are each independently selected from hydrogen, halogen, hydroxyl, amino, alkyl, alkenyl, alkynyl, aryl, benzyl, alkoxy, alkylthioxy, alkyl sulfonyl, alkyl sulfoxy, alkyl thio or any cyclic version or heteroatom containing version thereof and wherein for each alkyl, alkenyl, alkynyl, aryl, benzyl, alkoxy, alkylthioxy, alkyl sulfonyl, alkyl sulfoxy, alkyl thio and any cyclic version or heteroatom containing version may be substituted or unsubstituted; R3 is selected from hydrogen, halogen, hydroxyl, amino, alkyl, alkenyl, alkynyl, aryl, benzyl, alkoxy, alkylthioxy, alkyl sulfonyl, alkyl sulfoxy, alkyl thio or any cyclic version or heteroatom containing version thereof and wherein for each alkyl, alkenyl, alkynyl, aryl, benzyl, alkoxy, alkylthioxy, alkyl sulfonyl, alkyl sulfoxy, alkyl thio and any cyclic version or heteroatom containing version may be substituted or unsubstituted; and R4 and R5 are independently selected from hydrogen, amino, alkyl, alkenyl, alkynyl, aryl, benzyl, or any cyclic version or heteroatom containing version thereof and wherein for each alkyl, alkenyl, alkynyl, aryl, benzyl, and any cyclic version or heteroatom containing version may be substituted or unsubstituted; or R4 and R5 may be taken together to form a cyclic substituent, wherein the cyclic substituent may be aromatic or non aromatic and may further include one or more additional hetero atoms selected from O, S and N.
地址 Boxmeer NL