呋喃,2-(二氯甲基)四氢- | 931-05-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢呋喃
• 中文名称: 呋喃,2-(二氯甲基)四氢-
• 英文名称: 2-Dichlormethyl-tetrahydrofuran
• 英文别名: 2-(dichloromethyl)tetrahydrofuran；2-(dichloromethyl)oxolane
• CAS: 931-05-5
• 化学式: C₅H₈Cl₂O
• 分子量: 155.024
• InChiKey: LRRYUPYELLDERY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  8
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  9.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  2-(dichloromethyl)-2-hydroxytetrahydrofuran 在 三乙基硅烷 、 三氟化硼乙醚 、 碳酸氢钠 作用下， 以65%的产率得到呋喃,2-(二氯甲基)四氢-
  参考文献：
  名称：

  Reactivity of in situ generated dihalomethyllithium towards dicarboxylic acid diesters and lactones: Synthetic applications

  摘要：

  The reaction of dicarboxylic acid diesters 1, with in situ generated dihalomethyllithium (1:1.4 molar ratio) at -78-degrees-C leads, after hydrolysis, to the corresponding dihalomethylketoesters 3. The same process using an excess of the carbenoid (1:4 molar ratio) yields the expected tetrahalodiketones 5. The reaction of these carbenoids with gamma- and delta-lactones 6 at -78-degrees-C yields, after hydrolysis, 2-(dihalomethyl) gamma- or delta-lactols 7 or 8, respectively. The reaction of lactols 7 or 8 with triethylsilane or allyltrimethylsilane in the presence of BF3.OEt2 affords the corresponding substituted tetrahydrofurans or pyrans 10 or 12. The use of epsilon-caprolactone as starting material in the reaction with dihalomethyllithium leads to the corresponding 1,1-dihalo-7-hydroxy-2-heptanones.

  DOI：

  10.1016/s0040-4020(01)81943-8

文献信息

• [EN] PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF<br/>[FR] INHIBITEURS DE PROTÉINE TYROSINE PHOSPHATASE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：CALICO LIFE SCIENCES LLC

  公开号：WO2020186199A1

  公开（公告）日：2020-09-17

  Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders and conditions favorably responsive to PTPN 1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.

  本文提供了用于抑制蛋白酪氨酸磷酸酶的化合物、组合物和方法，例如蛋白酪氨酸磷酸酶非受体型2（PTPN2）和/或蛋白酪氨酸磷酸酶非受体型1（PTPN1），以及用于治疗对PTPN1或PTPN2抑制剂治疗有良好反应的相关疾病、紊乱和状况的方法，例如癌症或代谢性疾病。
• 2-aryl indole derivatives and their use as therapeutic agents
  申请人：——

  公开号：US20010039286A1

  公开（公告）日：2001-11-08

  The present invention relates compounds of the formula (I): 1 wherein R 1a , R 1b ; and R 2 represent a variety of substituents; R 3 represents an optionally substituted phenyl, biphenyl or naphthyl or heteroaryl group; R 4 represents hydrogen, C 1-6 alkyl, carbonyl (=O), (CH 2 ) p phenyl or a C 1-2 alkylene bridge across the piperidine ring; R 5 and R 6 each independently represent a variety of substituents; or R 5 and R 6 together are linked so as to form an optionally substituted 5-or 6-membered ring; X represents an oxygen or a sulfur atom, two hydrogen atoms, ═NH or ═N(C 1-6 alkyl); Y is a straight or branched C 1-4 alkylene, C 2-4 alkenylene or C 2-4 alkynylene chain; the dotted line represents an optional double bond; m is zero or an integer from 1 to 4; n is an integer from 1 to 4; and p is an integer from 1 to 4; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

  本发明涉及以下式（I）的化合物： 1 其中 R 1a ，R 1b ; 和 R 2 代表各种取代基; R 3 代表可选择地取代的苯基、联苯基或萘基或杂环芳基; R 4 代表氢、C 1-6 烷基、羰基（=O）、（CH 2 ） p 苯基或穿过哌啶环的 C 1-2 烷基桥; R 5 和 R 6 各自独立地代表各种取代基; 或 R 5 和 R 6 一起连接以形成可选择地取代的5-或6-成员环; X代表氧或硫原子、两个氢原子、═NH或═N(C 1-6 烷基); Y是直链或支链C 1-4 烷基、C 2-4 烯基或C 2-4 炔基链; 虚线表示可选的双键; m为零或1至4的整数; n为1至4的整数; p为1至4的整数; 或其药学上可接受的盐。 这些化合物在治疗或预防抑郁症、焦虑、疼痛、炎症、偏头痛、呕吐或带状疱疹后神经痛方面特别有用。
• Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
  申请人：Link T. James

  公开号：US20050277647A1

  公开（公告）日：2005-12-15

  The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

  本发明涉及抑制11-β-羟基类固醇脱氢酶1型酶的化合物。本发明还涉及利用11-β-羟基类固醇脱氢酶1型酶的抑制剂治疗非胰岛素依赖型2型糖尿病、胰岛素抵抗、肥胖、脂质紊乱、代谢综合征以及其他由过度糖皮质激素作用介导的疾病和症状。
• TRICYCLIC PIPERAZINE DERIVATIVE
  申请人：Sunovion Pharmaceuticals Inc.

  公开号：US20160083391A1

  公开（公告）日：2016-03-24

  Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same.

  揭示了作为磷酸二酯酶1（PDE1）抑制剂有用的化合物，以及它们的组合物和使用方法。
• Rifamycin analogs and uses thereof
  申请人：van Duzer H. John

  公开号：US20050043298A1

  公开（公告）日：2005-02-24

  The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′-and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.

  这项发明涉及利福霉素类似物，可用作治疗或预防各种微生物感染的治疗药物。在一种形式中，这些类似物在25位点上乙酰化，就像利福霉素一样。在另一种形式中，这些类似物在25位点上去乙酰化。在其他形式中，苯并噁唑利福霉素、苯并噻唑利福霉素和苯并二唑利福霉素类似物在苯环的各个位置上进行衍生化，包括3'-羟基类似物、4'-和/或6'卤代和/或烷氧基类似物，以及各种包含环胺基团的5'取代基。