| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 保护酚基 | CN201480029830.5 | 2014-05-12 | CN105308007A | 2016-02-03 | J·C·哈伦; S·D·布朗 |
| 提供一种保护前体化合物上的酚基的方法。所述方法包括使所述酚基在酸催化的保护反应中与二氢吡喃反应并且在小于约60秒内用强碱淬灭所述保护反应，形成受保护的前体化合物。 | ||||||
| 2 | 羟基保护化剂和羟基保护方法 | CN201280056101.X | 2012-11-16 | CN103987702A | 2014-08-13 | 国嶋崇隆; 藤田光; 山田耕平 |
| 本发明目的在于提供一种羟基保护化剂，其稳定而容易使用，没有致癌性或催泪性等，价格便宜；还提供一种能在酸性条件下保护羟基的羟基保护方法。技术方案是：羟基保护化剂是含氮的吸电子性的杂环藉氧原子、硫原子、氮原子当中任意一者而键合有一个以上保护基的羟基保护化剂。杂环譬如是三嗪环，保护基譬如是苄基。具体而言是2,4,6-三苄氧基-1,3,5-三嗪或2,4,6-三(4-甲氧基苄氧基)-1,3,5-三嗪等。此外也可使用2,4,6-三(叔丁氧基)-1,3,5-三嗪等。进行羟基保护之际，在酸性条件下使羟基保护化剂与具有羟基的对象化合物反应。 | ||||||
| 3 | 光学活性的哌嗪化合物的制造方法 | CN201010592276.5 | 2006-09-25 | CN102153620A | 2011-08-17 | 前田比吕志; 松井浩三; 板谷信重 |
| 本发明涉及光学活性的哌嗪化合物的制造方法。本发明提供一种式(11)表示的光学活性的1-甲基-3-苯基哌嗪或其盐的制造方法，其包括以下工序1～工序4、或者包括以下工序5～工序7以及工序4，还提供经由该方法制造光学活性的米氮平的方法。 | ||||||
| 4 | 保护酚基 | CN201480029830.5 | 2014-05-12 | CN105308007B | 2017-07-21 | J·C·哈伦; S·D·布朗 |
| 提供一种保护前体化合物上的酚基的方法。所述方法包括使所述酚基在酸催化的保护反应中与二氢吡喃反应并且在小于约60秒内用强碱淬灭所述保护反应，形成受保护的前体化合物。 | ||||||
| 5 | 氨基酸产生剂和含有氨基酸产生剂的聚硅氧烷组合物 | CN200980118183.4 | 2009-05-19 | CN102037092B | 2014-07-02 | 加藤拓; 小林淳平; 高野聪子; 作本直树 |
| 本发明的目的在于提供一种其氨基的保护基团脱去后会生成氨基酸的氨基酸产生剂，以及使用该氨基酸产生剂和含有该氨基酸产生剂的聚硅氧烷组合物的用于形成被膜的组合物。本发明提供了含有(A)成分、(B)成分和(C)成分的用于形成被膜的组合物。其中(A)成分是下述式(1)所示的氨基的保护基团脱去后会生成氨基酸的氨基酸产生剂，(B)成分是水解性硅烷、其水解物、其水解缩合物、或它们的混合物，(C)成分是溶剂。D-A？？式(1)(式中，D表示氨基的保护基团，A表示氨基酸去掉氨基的氢原子后所得的有机基团。) | ||||||
| 6 | 环烷二羧酸单酯的制造方法 | CN201080060034.X | 2010-11-25 | CN102686551A | 2012-09-19 | 大川春树 |
| 一种环烷二羧酸单酯的制造方法，其特征在于，包含：利用Z表示的基团对式（1-A）表示的化合物的2个羧基（-COOH）进行保护来获得式（2-A）表示的化合物的第一工序，和利用酸对第一工序中得到的式（2-A）表示的化合物的Z表示的基团中的任一个进行脱保护来获得式（3-A）表示的化合物的第二工序。（式中，m表示0~3的整数，p表示0或者1，Z表示甲硫基甲基等，R5、R6和R7各自独立地表示氢原子、碳原子数为1~8的烷基、碳原子数为1~8的烷氧基、苯基或者苄基）。 | ||||||
| 7 | 光学活性的哌嗪化合物的制造方法 | CN201010601788.3 | 2006-09-25 | CN102126978A | 2011-07-20 | 前田比吕志; 松井浩三; 板谷信重 |
| 本发明涉及光学活性的哌嗪化合物的制造方法。本发明提供一种式(11)表示的光学活性的1-甲基-3-苯基哌嗪或其盐的制造方法，其包括以下工序1～工序4、或者包括以下工序5～工序7以及工序4，还提供经由该方法制造光学活性的米氮平的方法。 | ||||||
| 8 | 制造2‑氨基取代苯甲醛化合物的方法 | CN201580044966.8 | 2015-08-25 | CN106573874A | 2017-04-19 | 小林真一 |
| 根据本发明，可提供一种制造氨基键合于2位、卤代基或烷氧基键合于3位且氢原子、烷基、卤代基、烷氧基或氰基各自独立地键合于4位、5位和6位的苯甲醛的方法，包括：准备卤代基或烷氧基键合于3位、氢原子键合于2位且氢原子、烷基、卤代基、烷氧基或氰基以锂化反应在2位最具活性的方式各自独立地键合于4位、5位和6位的苯甲醛，对该苯甲醛中的甲酰基进行缩醛保护，对2位依次进行锂化、叠氮化和氨基化，接着，进行缩醛脱保护。 | ||||||
| 9 | 环烷二羧酸单酯的制造方法 | CN201080060034.X | 2010-11-25 | CN102686551B | 2014-11-12 | 大川春树 |
| 一种环烷二羧酸单酯的制造方法，其特征在于，包含：利用Z表示的基团对式（1-A）表示的化合物的2个羧基（-COOH）进行保护来获得式（2-A）表示的化合物的第一工序，和利用酸对第一工序中得到的式（2-A）表示的化合物的Z表示的基团中的任一个进行脱保护来获得式（3-A）表示的化合物的第二工序。（式中，m表示0~3的整数，p表示0或者1，Z表示甲硫基甲基等，R5、R6和R7各自独立地表示氢原子、碳原子数为1~8的烷基、碳原子数为1~8的烷氧基、苯基或者苄基。） | ||||||
| 10 | 保护基所结合的羟基的脱保护方法 | CN201280018337.4 | 2012-04-19 | CN103492349A | 2014-01-01 | 石桥雄一郎; 松村靖 |
| 本发明是在不影响对酸不稳定的官能基的情况下对被叔丁基二甲基甲硅烷基保护的醇羟基进行脱保护。在溶剂存在下，对羟基被叔丁基二甲基甲硅烷基保护的醇的叔丁基二甲基甲硅烷基在下述条件下进行脱保护，即、在水中的pKa为1.0以上且3.0以下的酸或酸性盐的存在下进行脱保护。 | ||||||
| 11 | 光学活性的哌嗪化合物的制造方法 | CN201010601630.6 | 2006-09-25 | CN102126982A | 2011-07-20 | 前田比吕志; 松井浩三; 板谷信重 |
| 本发明涉及光学活性的哌嗪化合物的制造方法。本发明提供一种式(11)表示的光学活性的1-甲基-3-苯基哌嗪或其盐的制造方法，其包括以下工序1～工序4、或者包括以下工序5～工序7以及工序4，还提供经由该方法制造光学活性的米氮平的方法。 | ||||||
| 12 | 氨基酸产生剂和含有氨基酸产生剂的聚硅氧烷组合物 | CN200980118183.4 | 2009-05-19 | CN102037092A | 2011-04-27 | 加藤拓; 小林淳平; 高野聪子; 作本直树 |
| 本发明的目的在于提供一种其氨基的保护基团脱去后会生成氨基酸的氨基酸产生剂，以及使用该氨基酸产生剂和含有该氨基酸产生剂的聚硅氧烷组合物的用于形成被膜的组合物。本发明提供了含有(A)成分、(B)成分和(C)成分的用于形成被膜的组合物。其中(A)成分是下述式(1)所示的氨基的保护基团脱去后会生成氨基酸的氨基酸产生剂，(B)成分是水解性硅烷、其水解物、其水解缩合物、或它们的混合物，(C)成分是溶剂。D-A 式(1)(式中，D表示氨基的保护基团，A表示氨基酸去掉氨基的氢原子后所得的有机基团。)。 | ||||||
| 13 | 制备R－1－(芳氧基)丙－2－醇的方法 | CN01808380.3 | 2001-04-20 | CN1438981A | 2003-08-27 | J·F·拉罗 |
| 提供了一种制备(R)－1－(2，3－二氟－6－硝基苯氧基)－丙－2－醇的方法，该化合物在广泛使用的抗生素左氟沙星的合成中为有用的中间体。还描述了制备(R)－1－(2，3－二氟－6－硝基苯氧基)－2－三甲基甲硅烷氧基丙烷的方法。该方法包括在旋光Co(salen)催化剂存在下用2，3－二氟－6－硝基苯基三甲基甲硅烷基醚对(R)－环氧丙烷进行开环。反应物的三甲基甲硅烷基被转化成产物芳氧基醇，其用于就地保护仲醇。在分离时除去三甲基甲硅烷基并将所得区域异构体混合物提纯而以高纯度和高产率得到所需的(R)－1－(2，3－二氟－6－硝基苯氧基)－丙－2－醇。 | ||||||
| 14 | PROCESS FOR PRODUCING NOVEL 4-BENZOAZONINE DERIVATIVES | US15755275 | 2016-08-26 | US20180258047A1 | 2018-09-13 | Taizo ITO; Xiaoming LIAO; Zihua LI |
| An object of the present invention is to provide a novel tetrahydroazepine compound and a process for producing the same.The present invention relates to a tetrahydroazepine compound represented by the formula (10) or a salt thereof, anda process for producing the said compound or a salt thereof. (In the formula, R1 is an optionally substituted alkyl group, R2 is an optionally substituted alkyl group and one of the X—Y bond and the Y—Z bond is a carbon-carbon double bond and the other is a carbon-carbon single bond.) | ||||||
| 15 | Method for producing 2-amino-substituted benzaldehyde compound | US15504499 | 2015-08-25 | US10047037B2 | 2018-08-14 | Shinichi Kobayashi |
| The present invention provides a method for producing a benzaldehyde in which an amino group is bonded in the 2 position, a halogeno group or an alkoxy group is bonded in the 3 position, and a hydrogen atom, an alkyl group, a halogeno group, an alkoxy group, or a cyano group is bonded independently in each of the 4, 5, and 6 positions, the method including: preparing a benzaldehyde in which a halogeno group or an alkoxy group is bonded in the 3 position, a hydrogen atom is bonded in the 2 position, and a hydrogen atom, an alkyl group, a halogeno group, an alkoxy group, or a cyano group is bonded independently in each of the 4, 5, and 6 positions so that a lithiation reaction is most active at the 2 position; acetal-protecting a formyl group in the benzaldehyde; sequentially performing lithiation, azidation, and amination of the 2 position; and the performing acetal deportection. | ||||||
| 16 | SYNTHESIS OF CYCLOPROPYL INDOLES AND CYCLOHEPTA[B]INDOLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHOD OF USING THEM | US15545858 | 2015-12-03 | US20180002318A1 | 2018-01-04 | Weiping Tang; Xiaoxun Li |
| Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(l)-containing catalyst. | ||||||
| 17 | NOVEL CYCLIC DEPSIPEPTIDE DERIVATIVES AND HARMFUL ORGANISM CONTROL AGENTS COMPRISING THE SAME | US15488944 | 2017-04-17 | US20170215422A1 | 2017-08-03 | Masaaki MITOMI; Masayo SAKAI; Ryo HORIKOSHI; Yasumichi ONOZAKI; Satoshi NAKAMURA; Satoshi OMURA; Toshiaki SUNAZUKA; Tomoyasu HIROSE; Kazuro SHIOMI; Rokuro MASUMA |
| An objective of the present invention is to provide novel cyclic depsipeptide derivatives and harmful organism control agents including the same as each other. Specifically, the present invention provides compounds represented by formula (1) or stereoisomers thereof, harmful organism control agents containing them, and a process for producing them. | ||||||
| 18 | METHOD FOR PRODUCING DIPEPTIDE DERIVATIVE CONTAINING DISUBSTITUTED AMINO ACID RESIDUE | US14914458 | 2014-08-20 | US20160207958A1 | 2016-07-21 | Keisuke MATSUYAMA; Kazuya KODAMA |
| A method for producing a dipeptide that has a protected N-terminal and is represented by formula (1) or a salt of the dipeptide, said method comprising condensing an α-monosubstituted amino acid that has a protected N-terminal and is represented by formula (2) or glycine or a salt thereof with a disubstituted amino acid that is represented by formula (3) or a salt thereof in the presence of a condensing agent [in each of the formulae, substituents are as defined in the description or the like]. | ||||||
| 19 | Method for protecting hydroxyl or amine or thiol functions, novel compounds with protected hydroxyl or amine or thiol groups, as well novel compounds for the implementation of this method | US14396474 | 2013-04-23 | US09290521B2 | 2016-03-22 | Wojciech Tadeusz Markiewicz; Marcin Krzysztof Chmielewski; Sylwia Maria Musial; Hieronim Franciszek Maciejewski; Grzegorz Hreczycho |
| A novel method of simultaneously protecting two functions which are same or different, namely hydroxyl, amine, or thiol ones, particularly in sugars, polyalcohols, nucleosides, nucleotides, peptides, and nucleic acids during an organic synthesis, and to novel compounds for implementing this method, as well as to the method of obtaining these compounds. Method of simultaneously protecting two hydroxyl, amine, or thiol functions according to the invention by carrying out a protecting reaction between a compound having at least two free hydroxyl, amine, or thiol groups, and the disilane of formula 1, where R stands for Cl or Br, or I, or a substituent of formula 2, where X1, X2, X3, X4 are the same or different. | ||||||
| 20 | Production method for compound comprising amino group and/or hydroxyl group | US14382455 | 2013-03-04 | US09278905B2 | 2016-03-08 | Takashi Ohshima; Hiroyuki Morimoto; Yuhei Shimizu |
| Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A-NH2 (I). | ||||||
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