[(3S)-oxolan-3-yl] N-[(2S,3S)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: [(3S)-oxolan-3-yl] N-[(2S,3S)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
• 化学式: C₂₅H₃₅N₃O₆S
• 分子量: 505.6
• InChiKey: YMARZQAQMVYCKC-XWGVYQGASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  35
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  140
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• PROCESS FOR SYNTHESIS OF SYN AZIDO EPOXIDE AND ITS USE AS INTERMEDIATE FOR THE SYNTHESIS OF AMPRENAVIR & SAQUINAVIR
  申请人：Council of Scientific & Industrial Research

  公开号：US20150011782A1

  公开（公告）日：2015-01-08

  Disclosed herein is a novel route of synthesis of syn azide epoxide of formula 5, which is used as a common intermediate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt-catalyzed hydrolytic kinetic resolution of racemic anti-(2SR,3SR)-3-azido-4-phenyl-1,2-epoxybutane (azido-epoxide).

  本文披露了一种合成公式5的syn叠氮环氧化物的新路线，该化合物被用作HIV蛋白酶抑制剂的不对称合成的常见中间体，如Amprenavir、Fosamprenavir、Saquinavir以及通过钴催化的拆分手性反式-(2SR,3SR)-3-叠氮-4-苯基-1,2-环氧丁烷(叠氮环氧化物)合成Darunavir和Palinavir。
• [EN] PROCESS FOR THE PREPARATION OF SULFONAMIDES USEFUL AS RETROVIRAL PROTEASE INHIBITORS<br/>[FR] PROCÉDÉ DE PRÉPARATION DE SULFONAMIDES UTILES EN TANT QU'INHIBITEURS DE PROTÉASE RÉTROVIRAUX
  申请人：RANBAXY LAB LTD

  公开号：WO2013011485A1

  公开（公告）日：2013-01-24

  The present invention relates to a process for the preparation of sulfonamides useful as retroviral protease inhibitors.

  本发明涉及一种用于制备作为逆转录病毒蛋白酶抑制剂有用的磺胺类化合物的方法。
• A NOVEL PROCESS TO PREPARE INTERMEDIATES OF HIV-PROTEASE INHIBITORS THEREOF
  申请人：ZCL Chemicals Ltd.

  公开号：EP2998291A1

  公开（公告）日：2016-03-23

  The present invention relates to an industrially feasible and economically viable process for the preparation of (1S,2R)-3-[[4-aminophenyl)-sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenyl-methyl)propyl] amine of formula I and its salt thereof and optionally converting it to HIV-protease inhibitors like Darunavir, Amprenavir or its prodrug Fosamprenavir.

  本发明涉及一种工业可行且经济可行的过程，用于制备公式I中的(1S,2R)-3-[[4-氨基苯基)-磺酰基](2-甲基丙基)氨基]-2-羟基-1-(苯甲基)丙基]胺及其盐，并可选择将其转化为HIV蛋白酶抑制剂，如达芦那韦、安普那韦或其前药福安那韦。
• Composition and method to prevent or reduce diarrhea and steatorrhea in HIV patients
  申请人：SIPOS TIBOR

  公开号：US20100021505A1

  公开（公告）日：2010-01-28

  Method of preventing or reducing diarrhea and/or steatorrhea in HIV-positive patients being treated with High Activity Antiretroviral drugs containing protease inhibitors, nucleoside reverse transcriptase inhibitors or non-nucleoside reverse transcriptase inhibitors. The method includes the steps of: administering to the HIV-positive patient a High Activity Antiretroviral drug containing a protease inhibitor, a nucleoside reverse transcriptase inhibitor or a non-nucleoside reverse transcriptase inhibitor; and co-administering with the HAART drug a gastric acid-resistant polymer-coated and buffered digestive enzyme composition containing pancreatic proteases, lipases, co-lipases, nucleases, amylases and other bio-active substances produced by the pancreatic gland.

  预防或减少HIV阳性患者在接受含有蛋白酶抑制剂、核苷酸反转录酶抑制剂或非核苷酸反转录酶抑制剂的高活性抗逆转录病毒药物治疗时出现腹泻和/或脂肪泻的方法。该方法包括以下步骤：给HIV阳性患者口服含有蛋白酶抑制剂、核苷酸反转录酶抑制剂或非核苷酸反转录酶抑制剂的高活性抗逆转录病毒药物；同时与HAART药物联合给予一种胃酸耐受性聚合物包膜和缓冲的消化酶组合物，其中包含胰蛋白酶、脂肪酶、胆脂酶、核酸酶、淀粉酶和胰腺分泌的其他生物活性物质。
• Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds
  申请人：Arimilli N. Murty

  公开号：US20070010489A1

  公开（公告）日：2007-01-11

  Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit 5 HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.

  本发明揭示了具有HIV蛋白酶抑制剂性质的膦酸酯取代化合物，其具有作为治疗剂和其他工业用途的用途。该组合物抑制5型HIV蛋白酶活性和/或在治疗艾滋病和其他抗病毒感染方面具有治疗作用，以及在检测HIV蛋白酶方面的检测中有用。