(1S-cis)-4-Amino-2-cyclopentene-1-methanol D-hydrogen tatrate

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (1S-cis)-4-Amino-2-cyclopentene-1-methanol D-hydrogen tatrate
• 英文别名: (4-aminocyclopent-2-en-1-yl)methanol;2,3-dihydroxybutanedioic acid
• 化学式: C10H17NO7
• 分子量: 263.24
• InChiKey: LTSTZOJHLZNDFG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.24
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  161
• 氢给体数：
  6
• 氢受体数：
  8

文献信息

• Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4-((2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1- methanol
  申请人：Lonza AG

  公开号：US20020010360A1

  公开（公告）日：2002-01-24

  The invention relates to a novel process for the preparation of an aminoalcohol of the formula 1 racemically or optically active, starting from 2-azabi-cyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae 2 In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formula 3 to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae 4 and then cyclized to give the end compounds.

  该发明涉及一种新颖的方法，用于制备公式1的氨基醇，其为外消旋或光学活性，从2-azabi-cyclo［2.2.1］hept-5-en-3-one出发，进一步转化为相应的酰基衍生物，再进一步转化为公式2中的(1S,4R)-或(1R,4S)-4-(2-氨基-6-氯-9-H-嘌呤-9-基)-2-环戊烯基-1-甲醇。在后一合成中，氨基醇转化为相应的D-或L-酒石酸盐，然后与公式3中的N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺反应，以得到公式4中的(1S,4R)-或(1R,4S)-4-(2-氨基-6-氯-5-甲酰胺基-4-嘧啶基)氨基-2-环戊烯基-1-甲醇，然后进行环化反应以得到最终的化合物。
• Process for the preparation of aminoalcohol derivatives and their further conversion to (1R,4S)-4-(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol
  申请人：——

  公开号：US20040142436A1

  公开（公告）日：2004-07-22

  The invention relates to a novel process for the preparation of an aminoalcohol of the formula 1 racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae 2 In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) form amide of the formula 3 to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae 4 and then cyclized to give the end compounds.

  本发明涉及一种从2-氮杂双环[2.2.1]庚-5-烯-3-酮出发制备公式1的氨基醇的新工艺，其进一步转化为相应的酰基衍生物，并进一步转化为公式2的(1S,4R)-或(1R,4S)-4-(2-氨基-6-氯-9-H-嘌呤-9-基)-2-环戊基-1-甲醇。在后一种合成中，氨基醇转化为相应的D-或L-酒石酸盐，然后与公式3的N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺反应，以给出公式4的(1S,4R)-或(1R,4S)-4-[(2-氨基-6-氯-5-甲酰基-4-嘧啶基)氨基]-2-环戊基-1-甲醇，然后环化以得到最终产物。
• PROCESS FOR THE PREPARATION OF AMINOALCOHOL DERIVATIVES AND THEIR FURTHER CONVERSION TO (1R, 4S)-4(2-AMINO-6-CHLORO-5-FORMAMIDO-4- PYRIMIDINYL)-AMINO-2-CYCLOPENTENYL-1-METHANOL
  申请人：Brieden Walter

  公开号：US20060211862A1

  公开（公告）日：2006-09-21

  The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or ( 1 R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formula to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

  本发明涉及一种新型的制备氨基醇的方法，该氨基醇的结构式为，可以是外消旋或内消旋，从2-氮杂双环[2.2.1]庚-5-烯-3-酮开始，进一步转化为相应的酰基衍生物，然后进一步转化为(1S,4R)-或(1R,4S)-4-(2-氨基-6-氯-9-H-嘌呤-9-基)-2-环戊烯基-1-甲醇，其结构式为。在后一种合成中，氨基醇转化为相应的D-或L-酒石酸盐，然后与N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺反应，其结构式为，以给出(1S,4R)-或(1R,4S)-4-[(2-氨基-6-氯-5-甲酰基-4-嘧啶基)氨基]-2-环戊烯基-1-甲醇，其结构式为，然后环化以得到最终化合物。
• US6448402B2
  申请人：——

  公开号：US6448402B2

  公开（公告）日：2002-09-10
• US6723868B1
  申请人：——

  公开号：US6723868B1

  公开（公告）日：2004-04-20