Macrocin

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Macrocin
• 英文别名: 2-[(4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-[(2R,3R,4R,5S,6R)-5-[(2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-15-[[(2R,3R,4R,5S,6R)-4,5-dihydroxy-3-methoxy-6-methyloxan-2-yl]oxymethyl]-16-ethyl-4-hydroxy-5,9,13-trimethyl-2,10-dioxo-1-oxacyclohexadeca-11,13-dien-7-yl]acetaldehyde
• 化学式: C₄₅H₇₅NO₁₇
• 分子量: 902.1
• InChiKey: UFUYRGNJTFAODM-HQCAVAADSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  63
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.84
• 拓扑面积：
  250
• 氢给体数：
  6
• 氢受体数：
  18

反应信息

• 作为反应物：
  描述：

  Macrocin 、 (3S,5R)-3,5-dimethylpiperidine 、 甲醇 、 氰基硼氢化钠 以64%的产率得到
  参考文献：
  名称：

  DEBONO, MANUEL;WILLARD, KEVIN E.;KIRST, HERBERT A.;WIND, JULIE A.;CROUSE,+, J. ANTIBIOTICS, 42,(1989) N, C. 1253-1267

  摘要：

  DOI：

文献信息

• [EN] BRIDGED MACROCYCLIC COMPOUNDS AND PROCESSES FOR THE PREPARATION THEREOF<br/>[FR] COMPOSES MACROCYCLIQUES PONTES ET PROCEDES DE PREPARATION DESDITS COMPOSES
  申请人：ENANTA PHARM INC

  公开号：WO2005080408A1

  公开（公告）日：2005-09-01

  The present invention provides a method for preparing bridged macrocyclic compounds comprising the step of reacting a macrocyclic compound characterized by having at least two nucleophilic moieties with a bifunctional bridging reagent optionally in the presence of a catalyst, thereby producing a bridged macrocyclic product.

  本发明提供了一种制备桥联大环化合物的方法，包括以下步骤：将至少具有两个亲核基团的大环化合物与双功能桥接试剂反应，可选地在催化剂的存在下进行，从而产生桥联大环产物。
• Macrolide solid-state forms
  申请人：Intervet International BV

  公开号：EP2019112A1

  公开（公告）日：2009-01-28

  This invention relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

  本发明涉及20,23-二哌啶基-5-O-链霉素基-泰龙环酮的溶剂化和非溶剂化晶体形式，以及制备这种晶体形式的方法，包含或来源于这种晶体形式的药物，制备包含或来源于这种晶体形式的药物的方法，使用这种晶体形式进行治疗的方法以及包含这种晶体形式的工具箱。
• Cloning vectors for use in Streptomyces
  申请人：ELI LILLY AND COMPANY

  公开号：EP0077649A2

  公开（公告）日：1983-04-27

  The present invention discloses selectable recombinant DNA cloning vectors comprising: a) a functional origin of replication containing restriction fragment of plasmid pEL103, and b) one or more DNA segments that convey resistance to at least one antibiotic when transformed into a sensitive host cell, said host cell being susceptible to transformation, cell division, and culture, for use in Streptomyces and related organisms.

  本发明公开了可选择的重组 DNA 克隆载体，该载体包括：a) 含有质粒 pEL103 限制性片段的功能性复制起源；b) 一个或多个 DNA 片段，当其转化到敏感的宿主细胞中时，可传递对至少一种抗生素的抗性，所述宿主细胞易于转化、细胞分裂和培养，用于链霉菌和相关生物。
• Mycaminosyl-tylonolide ester derivatives
  申请人：ELI LILLY AND COMPANY

  公开号：EP0082003A1

  公开（公告）日：1983-06-22

  Ester derivatives of 5-0-mycaminosyl tylonide (OMT) of the formula (I): wherein R and R1 are selected from hydrogen, optionally substituted Cl-C2-alkanoyl or optionally substituted benzoyl, phenylacetyl, or phenylproprionyl; R2 is mis 1 or 2. and R3 is 3-pyridyl or a group of the formula (I): where R5 and R6 are independently hydrogen, methyl, ethyl, methoxy, or nitro, X is O or S, and n is 0 or 1; provided that when R1 is other than hydrogen, R must also be other than hydrogen; and the pharmaceutically acceptable acid addition salts thereof; which are useful highly potent antibiotics, are provided.

  提供了式(I)为5-0-mycaminosyl tylonide (OMT)的酯类衍生物：其中R和R1选自氢、任选取代的Cl-C2-烷酰基或任选取代的苯甲酰基、苯乙酰基或苯丙酰基；R2为误1或误2；R3为3-吡啶基或式(I)的基团：其中R5和R6独立地为氢、甲基、乙基、甲氧基或硝基，X为O或S，n为0或1；但当R1不是氢时，R也必须不是氢；以及其药学上可接受的酸加成盐；它们是有用的高效抗生素。
• Cloning vectors
  申请人：ELI LILLY AND COMPANY

  公开号：EP0085548A2

  公开（公告）日：1983-08-10

  The present invention discloses multi-functional recombinant DNA cloning vectors comprising a) two or more functionally different origins of replication that are indpendently selected from the group consisting of any origin of replication that is functional in Streptomyces, any origin of replication that is functional in Bacillus, and any origin of replication that is functional in E. coli, and b) one or more DNA segments that confer resistance to at least one antibiotic when transformed into a sensitive host cell in which an origin of replication comprising said vector is functional, said host cells being susceptible to transformation, cell division, and culture, subject to the limitation that when. said vector is limited to two functionally different origins of replication, neither of the origins of replication is functional in E. coli.

  本发明公开了多功能重组DNA克隆载体，该载体包括：a)两个或多个功能不同的复制起源，这些复制起源可单独选自链霉菌中的任何功能性复制起源、芽孢杆菌中的任何功能性复制起源和大肠杆菌中的任何功能性复制起源组成的组；b)一个或多个DNA片段，当转化到敏感的宿主细胞中时，这些宿主细胞对至少一种抗生素具有抗性，在这些宿主细胞中，包含所述载体的复制起源是功能性的，所述宿主细胞易于转化、细胞分裂和培养，但当所述载体仅限于两个功能不同的复制起源时，这两个复制起源在大肠杆菌中都不是功能性的。