1350619-77-0

Basic information

• Product Name: Grazoprevir interMediate
• Synonyms: Grazoprevir interMediate;(1R,2R)-2-(4-Pentyn-1-yl)cyclopropanol;Cyclopropanol, 2-(4-pentyn-1-yl)-, (1R,2R)-;(1R,2R)-2-(pent-4-yn-1-yl)cyclopropan-1-ol;EOS-61021
• CAS NO: 1350619-77-0
• Molecular Formula: C8H12O
• Molecular Weight: 124.18028
• EINECS: -0
• Product Categories: intermediates
• Mol File: 1350619-77-0.mol

Chemical Properties

• Boiling Point: 186.3±13.0 °C(Predicted)
• Appearance: /
• Density: 1.025±0.06 g/cm3(Predicted)
• PKA: 15.26±0.40(Predicted)
• CAS DataBase Reference: Grazoprevir interMediate(CAS DataBase Reference)
• NIST Chemistry Reference: Grazoprevir interMediate(1350619-77-0)
• EPA Substance Registry System: Grazoprevir interMediate(1350619-77-0)

Safety Data

• Hazardous Substances Data: 1350619-77-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
Grazoprevir intermediate is used as a crucial component in the synthesis of grazoprevir for the treatment of chronic hepatitis C virus (HCV) infection. It plays a pivotal role in the manufacturing process, ensuring the production of the active pharmaceutical ingredient that forms the backbone of the final medication. This intermediate is essential for the development of effective treatments against HCV, contributing to the formulation of medications that can combat this viral infection.

Upstream product

• 126726-63-4 2-[2-(3-chloropropyl)cyclopropyl]-4,4,5,5-tetramethyl[1,3,2]dioxaborolane 
• 136835-38-6 (E)-2-(3-chloropropyl)-1-cyclopropanol 
• 154820-95-8 2-(5-chloropent-1-en-1-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 1224174-07-5 (S)-1-chlorohept-6-en-2-ol 

Downstream Products

• 1425038-19-2 (S)-3,3-dimethyl-2-(((1R,2R)-2-(pent-4-ynyl)cyclopropoxy)carbonylamino)butanoic acid 
• 1425038-21-6 (S)-3,3-dimethyl-2-((((1R,2R)-2-(pent-4-yn-1-yl)cyclopropoxy)carbonyl)amino)butanoic acid tert-butylamine salt 
• 1425038-23-8 methyl (1aR,5S,8S,10R,22aR)-5-tert-butyl-14-methoxy-3,6-dioxo-18,19-didehydro-1,1a,3,4,5,6,9,10,20,21,22,22a-dodecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3, 6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxylate 
• 1350514-68-9 grazoprevir 
• 1534367-64-0 C₄₁H₅₃N₅O₉S 
• 1449296-59-6 C₁₇H₂₂O₃ 

Relevant articles and documents

Asymmetric Synthesis of Functionalized trans-Cyclopropoxy Building Block for Grazoprevir

A practical and asymmetric synthesis of a functionalized trans-cyclopropoxy building block for the preparation of the HCV NS3/4a protease inhibitor grazoprevir is reported. Intramolecular SN2 displacement-ring closure, followed by a Baeyer-Villiger oxidation, yields the desired trans-cyclopropanol with full control of diastereoselectivity. A terminal alkyne is then effectively installed using LiNH(CH2)2NEt2. Starting from (S)-epichlorohydrin, the cyclopropoxy building block is prepared in 51% overall yield with >99.8% optical purity without isolation of any intermediates.

Process and intermediates for preparing macrolactams

The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

METHODS AND INTERMEDIATES FOR PREPARING MACROLACTAMS

The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

Inhibitors of nedd8-activating enzyme

The invention relates to an administration unit comprising crystalline form I of {(1 S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216) hydrochloride salt and to a packaging comprising the administration unit according to the invention.

CRYSTAL FORMS OF A HCV PROTEASE INHIBITOR

The present invention relates to different forms of a HCV inhibitory compound.