5-Thia-1-aza-bicyclo-<4.2.0>-oct-2-en-8-on | 55715-34-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 5-Thia-1-aza-bicyclo-<4.2.0>-oct-2-en-8-on
• 英文别名: Δ³-Cephem；5-thia-1-aza-bicyclo[4.2.0]oct-2-en-8-one；8-Oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene；5-thia-1-azabicyclo[4.2.0]oct-2-en-8-one
• CAS: 55715-34-9
• 化学式: C₆H₇NOS
• 分子量: 141.194
• InChiKey: FZEVMBJWXHDLDB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  45.6
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-hydroxy-5-thia-1-aza-bicyclo[4.2.0]octan-8-one 在 吡啶 、 对甲苯磺酰氯 作用下， 生成 5-Thia-1-aza-bicyclo-<4.2.0>-oct-2-en-8-on
  参考文献：
  名称：

  cepham衍生物的简单合成

  摘要：

  β-mercaptocarbonyl化合物与4-乙酰氧基-2-氮杂环丁酮缩合，得到4- hydroxycepham衍生物和从这些，根据各种方法，Δ 3 -cephem衍生物和Δ 3 -cephem本身制备。

  DOI：

  10.1002/jlac.197419740311

文献信息

• [EN] CEPHALOSPORIN INTERMEDIATE AND PROCESS FOR ITS PREPARATION<br/>[FR] PRODUIT INTERMÉDIAIRE DE CÉPHALOSPORINE ET SON PROCÉDÉ DE PRÉPARATION
  申请人：FRESENIUS KABI ANTI-INFECTIVES SRL

  公开号：WO2016128580A1

  公开（公告）日：2016-08-18

  Provided is a synthesis of cephalosporin derivatives, characterized by the use of the new intermediates for the preparation of cephalosporin derivatives, a crystalline toluene hemi-solvate of benzhydryl (6R,7R)-7β-[(phenylacetyl)amino]-3-[4-pyridyl-2-thiazolylthio]-3-cephem-4-carboxylate, and a crystalline 4-[2-[[(6R,7R)-7-amino-2 carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]-thio]-4-thiazolyl]-1-methyl-pyridinium chloride, hydrochloride (1:1:1), obtained by a specific process and processes for preparation thereof.

  提供了头孢菌素衍生物的合成，其特点是利用新中间体制备头孢菌素衍生物，一种结晶甲苯半溶剂的苄基(6R,7R)-7β-[(苯乙酰)氨基]-3-[4-吡啶基-2-噻唑基硫基]-3-头孢烯-4-羧酸酯，以及一种结晶4-[2-[[(6R,7R)-7-氨基-2-羧基-8-氧代-5-硫代-1-氮杂双环[4.2.0]辛-2-烯-3-基]-硫基]-4-噻唑基]-1-甲基吡啶盐酸盐，通过特定工艺获得，并制备的工艺。
• [EN] (--)- HUPERZINE A PROCESSES AND RELATED COMPOSITIONS AND METHODS OF TREATMENT<br/>[FR] PROCÉDÉS DE FABRICATION DE (-) HUPERZINE A, COMPOSITIONS ASSOCIÉES, ET MÉTHODES DE TRAITEMENT
  申请人：UNIV YALE

  公开号：WO2012121863A1

  公开（公告）日：2012-09-13

  The invention provides (1) processes for making substantially-pure (-) huperzine A and substantially-pure (-) huperzine A derivatives; (2) compositions useful in making substantially-pure (-) huperzine A and substantially-pure (-) huperzine A derivatives; and (3) methods of treating or preventing neurological disorders using substantially-pure (-) huperzine A and substantially-pure (-) huperzine A derivatives.

  该发明提供了三个方面：(1) 制备几乎纯的(-)华佩嗪A和几乎纯的(-)华佩嗪A衍生物的过程；(2) 用于制备几乎纯的(-)华佩嗪A和几乎纯的(-)华佩嗪A衍生物的组合物；以及(3) 使用几乎纯的(-)华佩嗪A和几乎纯的(-)华佩嗪A衍生物治疗或预防神经系统疾病的方法。
• Viral inhibitors
  申请人：Neyts Johan

  公开号：US20050239821A1

  公开（公告）日：2005-10-27

  The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine derivative having the general formula (Z): (formula). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.

  本发明涉及一种用于治疗或预防病毒感染的药物组合物，其包括至少一种具有通式（Z）的咪唑并[4,5-c]吡啶衍生物作为活性成分。本发明还涉及根据上述通式制备化合物的方法以及它们作为药物或用于治疗或预防病毒感染的用途。
• Cephalosporin derivatives, their preparation and compositions containing
  申请人：Rhone-Poulenc Sante

  公开号：US04508717A1

  公开（公告）日：1985-04-02

  Cephalosporin derivatives of the formula: ##STR1## in which A is a single bond or a radical --CH.sub.2 --, --NH-- or --NHCO--, attached to the 3-position or 4-position of the pyridinio radical, R is a methyl, carboxymethyl, carbamoylmethyl, benzyl or allyl radical, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or alternatively R.sub.a is carboxyl and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms or alkyl radicals, or together form an alkylene radical, and n equals 0 or 1, in their syn form, and also their addition salts with acids, metal salts and addition salts with nitrogen-containing bases are antibacterial agents having a broad spectrum of activity.

  化合物的头孢菌素衍生物的公式：##STR1## 其中A是连接到吡啶基的3位或4位的单键或基团--CH.sub.2 --，--NH--或--NHCO--，R是甲基，羧甲基，氨甲基，苄基或丙烯基基团，R.sub.a，R.sub.b和R.sub.c是氢原子，或者R.sub.a是羧基，R.sub.b和R.sub.c是相同或不同的氢原子或烷基基团，或者一起形成一个烷基基团，n等于0或1，在它们的同构体形式中，以及它们与酸，金属盐和含氮碱的加合物的加成盐是具有广泛活性的抗菌剂。
• Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment
  申请人：Bondy S. Steven

  公开号：US20050222198A1

  公开（公告）日：2005-10-06

  The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general formula (A): wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general formula and their use in the treatment or prophylaxis of viral infections.

  本发明涉及制备用于治疗或预防病毒感染的药物组合物，其包含至少一种具有通式（A）的咪唑[4,5-c]吡啶前药作为活性成分，其中取代基在规范中描述。本发明还涉及根据上述通式制备和筛选化合物的过程，以及它们在治疗或预防病毒感染中的用途。