(R)-N-(3-((4-Amino-6,7-dimethoxyquinazolin-2-yl)(methyl)amino)propyl)tetrahydrofuran-2-carboxamide | 123739-69-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: (R)-N-(3-((4-Amino-6,7-dimethoxyquinazolin-2-yl)(methyl)amino)propyl)tetrahydrofuran-2-carboxamide
• 英文别名: (2R)-N-[3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]propyl]oxolane-2-carboxamide
• CAS: 123739-69-5
• 化学式: C₁₉H₂₇N₅O₄
• 分子量: 389.4
• InChiKey: WNMJYKCGWZFFKR-CQSZACIVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  28
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• [EN] CATALYTIC HYDROGENATION OF NITRILES TO PRODUCE CAPSAICINOID DERIVATIVES AND AMINE COMPOUNDS, AND METHODS FOR PURIFIYING AND OBTAINING THE POLYMORPHS THEREOF<br/>[FR] HYDROGENATION CATALYTIQUE DE NITRILES POUR PRODUIRE DES DERIVES CAPSAICINOIDES ET DES COMPOSES D'AMINES, ET PROCEDES DE PURIFICATION ET D'OBTENTION DE LEURS POLYMORPHES
  申请人：STIEFEL LABORATORIES

  公开号：WO2005068414A1

  公开（公告）日：2005-07-28

  Processes for preparing an amine compound by catalytically hydrogenating a precursor nitrile compound. In a particular aspect, the present hydrogenation process occurs in a dipolar organic solvent in the presence of a palladium/carbon catalyst and a strong anhydrous protic acid. In a further aspect, the preferred embodiment relates to a process for deprotecting a compound to produce an amine compound. In yet a further aspect, the preferred embodiment relates to amine products produced by the present processes. These amine products may be used for a variety of purposes.

  通过在存在钯/碳催化剂和强无水质子酸的情况下，在偶极有机溶剂中催化氢化前体腈化合物的过程。在一个特定方面，目前的氢化过程发生在一个偶极有机溶剂中，在钯/碳催化剂和强无水质子酸的存在下。在另一个方面，首选实施例涉及一种去保护化合物以产生胺化合物的过程。在另一个方面，首选实施例涉及通过目前的过程产生的胺产品。这些胺产品可以用于各种目的。
• PREPARATION OF ALFUZOSIN
  申请人：Anumula Reddy Raghupathi

  公开号：US20070066824A1

  公开（公告）日：2007-03-22

  A process for preparing alfuzosin or a salt thereof, which minimizes the concentration of an N 1 -(4-amino-6,7-dimethoxyquinazolin-2-yl)-N 1 -methyl-N 2 -(4-amino-6,7-dimethoxyquinazolin-2-yl)-propane-1,3-diamine impurity in the product.

  一种制备奥法唑辛或其盐的方法，该方法可以最小化产品中N1-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-N1-甲基-N2-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-丙烷-1,3-二胺杂质的浓度。
• Use of Adrenergic N-Phenylpiperazine Antagonists, Pahrmaceutical Compositions Containning Them, and Methods of Preparing Them
  申请人：Soares Romeiro Antonio Luiz

  公开号：US20070219213A1

  公开（公告）日：2007-09-20

  The present invention describes phenylpiperazinyl alpha adrenergic antagonists that corresponds to the formula (I) which selectively act on the alpha 1A/alpha 1D subtypes, where its selectivity index in comparison to alpha 1B subtype is, at minimum, 1700 for the alpha 1A subtype and 10000 for the alpha 1 D subtype, being therefore useful for the treatment of the lower urinary tract symptoms, including the benign prostatic hyperplasia treatment in mammals, preferentially humans. It is also described pharmaceutical compositions containing said compounds and methods for its preparation.

  本发明描述了与公式（I）相对应的苯基哌嗪基α肾上腺素受体拮抗剂，其选择性作用于α1A/α1D亚型，其中与α1B亚型相比的选择性指数，对于α1A亚型至少为1700，对于α1D亚型至少为10000，因此可用于治疗哺乳动物，尤其是人类的下尿路症状，包括良性前列腺增生的治疗。还描述了含有该化合物的药物组合物以及其制备方法。
• Catalytic hydrogenation of nitriles to produce capsaicinoid derivatives and amine compounds, and methods for purifying and obtaining the polymorphs thereof
  申请人：Meckler Harold

  公开号：US20060047171A1

  公开（公告）日：2006-03-02

  Processes for preparing an amine compound by catalytically hydrogenating a precursor nitrile compound. In a particular aspect, the present hydrogenation process occurs in a dipolar organic solvent in the presence of a palladium/carbon catalyst and a strong anhydrous protic acid. In a further aspect, the preferred embodiment relates to a process for deprotecting a compound to produce an amine compound. In yet a further aspect, the preferred embodiment relates to amine products produced by the present processes. These amine products may be used for a variety of purposes.

  通过催化氢化前体腈化合物制备胺化合物的过程。在特定方面，本氢化过程发生在极性有机溶剂中，在钯/碳催化剂和强无水质子酸的存在下。在进一步方面，首选实施例涉及去保护化合物以产生胺化合物的过程。在另一个进一步方面，首选实施例涉及由本过程产生的胺产品。这些胺产品可用于各种用途。
• Composition comprising alfuzosin
  申请人：Cimex Pharma AG

  公开号：EP1637129A1

  公开（公告）日：2006-03-22

  A monolithic composition includes alfuzosin in a polymeric matrix adapted to release 13-33% of the alfuzosin within 2 hours, 40-60% of the alfuzosin within 7 hours, and greater than 80% of the alfuzosin within 20 hours of administration. A unit dosage form includes: a heterogeneous mixture of alfuzosin hydrochloride anhydrate, lactose monohydrate, hydroxypropylmethylcellulose, polyvinylpyrrolidone and magnesium stearate, wherein the heterogeneous mixture is heterogeneously distributed throughout the unit dosage form. A manufacturing process includes: mixing a hydrophilic polymer and alfuzosin to provide a blend; granulating the blend to provide granules; drying the granules on a dryer to provide dried granules; sizing the dried granules to provide sized granules; mixing the sized granules with a lubricant to obtain a mixture; and compressing the mixture to obtain a tablet. A method of treating benign prostatic hyperplasia, includes administering to a patient the composition or unit dosage form once a day.

  一种单片组合物包括聚合基质中的阿夫唑嗪，该聚合基质可在给药后 2 小时内释放 13-33%的阿夫唑嗪、7 小时内释放 40-60%的阿夫唑嗪、20 小时内释放 80%以上的阿夫唑嗪。一种单位剂型包括：盐酸阿夫唑嗪水合物、一水乳糖、羟丙基甲基纤维素、聚乙烯吡咯烷酮和硬脂酸镁的异质混合物，其中异质混合物异质分布在整个单位剂型中。一种生产工艺包括：混合亲水性聚合物和阿夫唑嗪，以得到混合物；将混合物制粒，以得到颗粒；在干燥器上干燥颗粒，以得到干燥颗粒；对干燥颗粒进行定型，以得到定型颗粒；将定型颗粒与润滑剂混合，以得到混合物；以及压缩混合物，以得到片剂。一种治疗良性前列腺增生症的方法，包括每天一次给患者服用组合物或单位剂型。