专利号:WO-0206209-A1 优先权日:2000-07-19 标 题 :Synthesis method for n1,n3-bis (2.aminoethyl) propane-1,3-diamine, synthesis intermediates, resulting products and use thereof in synthesis of cyclam 发明人:HANDEL HENRI; BERNARD HELENE; ANTOINE MARINE 权利人:UNIV BRETAGNE OCCIDENTALE; HANDEL HENRI; BERNARD HELENE; ANTOINE MARINE 摘要:The invention concerns a method of synthesis of a linear polynitrogen-containing derivative, namely N1,N3-bis (2-aminoethyl) propane-1,3-diamine of general formula (I) using as synthesis intermediates compounds (II) and (III). The invention also concerns the resulting products and their use in the synthesis of cyclic polynitrogen-containing derivatives such as cyclam.
专利号:US-4111933-A 优先权日:1976-04-30 标题:Protection of functional groups during reaction and their subsequent restoration 发明人:ECKERT HEINER; UGI IVAR; KABBE HANS-JOACHIM 权利人:BAYER AG 摘要:In the process for preparing an organic compound of the formula n n A' -- X n n in which n X is an amino group, a hydroxyl group or a carboxyl group, and n A' is the remainder of the molecule, from an organic compound of the formula n n A -- X n n in which n A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula n n A -- Z -- COOR n n in which n Z is --NH--, --O-- or a direct C--C bond, and n R is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CHâ•?CH-- group or an arylene group, n R 1 to R 4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or n R 1 + r 2 and R 3 + R 4 each independently completes a 5- or 6-membered carbocyclic ring, or n R 1 and R 3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, n Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula n n A' -- Z -- COOR n n and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporis.
专利号:WO-2023151188-A1 优先权日:2022-02-08 标题 :Green synthesis method of antiviral drug intermediate 发明人:XIA BIN; WANG JIAMING; ZHANG XIANSHU; CAI LINGLI; WANG ZIKUN; CAO MING; YANG SHAOBO; GAO QIANG; ZHENG BAOFU 权利人:SHANGHAI HAOYUAN CHEMEXPRESS CO LTD 摘要:The present application provides a green synthesis method of an antiviral drug intermediate. The method comprises: in the presence of a catalyst, adding zinc powder into a compound as represented by a formula II and performing a cyclization reaction with dihaloalkane to generate a compound as represented by a formula I, zinc halide being not required to be added to the cyclization reaction, wherein R1 is selected from H or an amino-protecting group, and R2 is selected from substituted or unsubstituted C1-C10 alkyl, substituted or unsubstituted C6-C14 aryl or substituted or unsubstituted C7-C14 aralkyl; R3 and R4 are each independently selected from hydrogen, substituted or unsubstituted C1-C10 alkyl, and R3 and R4 can be connected to form a fatty ring containing 3-10 carbon atoms. The synthesis method is short in steps, dangerous and expensive materials are not used, a reaction conversion rate is high, reaction time is short, and operation is easy and convenient. Production costs and post-treatment costs are reduced, and a cost advantage is obvious. The method can be widely used for preparing antiviral drugs of nirmatrelvir, boceprevir or narlaprevir, and has good market prospects.
专利号:US-6232318-B1 优先权日:1998-11-12 标 题:Pyrimidinedione derivatives useful as alpha 1A adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G 权利人:MERCK & CO LTD 摘要:Novel pyrimidinedione compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:WO-2024131056-A1 优先权日:2022-12-20 标 题:Synthesis method for intermediate of paxlovid and of boceprevir 发明人:YANG XIAOLONG; PEI PIBING; CHEN QIAN; YANG TIEBO; Yang Kaimike 权利人:HUANGGANG LUBAN PHARMACEUTICAL CO LTD 摘要:Disclosed in the present invention is a novel method for synthesizing a compound represented by formula 1. The method comprises: reacting diphenyl sulfide with 2-bromopropane to obtain a compound represented by formula 5; reacting a compound represented by formula 4 with the compound represented by formula 5 to obtain a compound represented by formula 6; and subjecting the compound represented by formula 6 to deprotection and salt forming under the effect of hydrogen chloride, so as to obtain the compound represented by formula 1. The method of the present invention can be carried out under mild conditions, thereby facilitating industrial production and further improving the reaction yield.
专利号:JP-2007521235-A 优先权日:2003-08-19 标题 :Method and apparatus for the synthesis of olefins, alcohols, ethers and aldehydes