24-hydroxy vitamin D derivatives

• US 6,538,145 B2
• Filed: 03/19/2002
• Issued: 03/25/2003
• Est. Priority Date: 02/24/1998
• Status: Expired due to Fees

• Current Assignee: Chugai Seiyaku Kabushiki Kaisha (Roche Holding AG)
• Original Assignee: Chugai Seiyaku Kabushiki Kaisha (Roche Holding AG)
• Inventors: Watanabe, Hiroyoshi, Hatakeyama, Susumi, Kawase, Akira
• Primary Examiner(s): QAZI, SABIHA NAIM
• Application Number:
  US10/099,987
• Publication Number:
  US 20020094972A1
• Time in Patent Office: 371 Days
• Field of Search: 552/653, 514/182, 514/167
• US Class Current: 552/653
• CPC Class Codes: C07C 2601/14 The ring being saturated
• CPC Class Codes: C07C 2602/24 the ring system containing nine carbon atoms, e.g. perhydroindane
• CPC Class Codes: C07C 33/44 containing rings other than six-membered aromatic rings
• CPC Class Codes: C07C 35/32 the condensed ring system being a (4.3.0) system, e.g. indenols
• CPC Class Codes: C07C 401/00 Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
• CPC Class Codes: C07F 7/1804 Compounds having Si-O-C linkages Si-O-acyl linkages C07F7/1896
• CPC Class Codes: Y02P 20/55 Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

A process for preparing vitamin D derivatives having the following formula:

wherein R₁, R₂, R₃, and R₄, which may be the same or different, represent a hydrogen atom or a protecting group, comprising:

reacting a compound of formula (2)

 wherein R₁ represents a hydrogen atom or a protecting group, with a compound having the formula (3)

 wherein R₁ represents a hydrogen atom and R₂, R₃, and R₄, which are the same or different, represent a hydrogen atom or a protecting group.

Claims

1. A process for preparing vitamin D derivatives having the following formula:

wherein R₁, R₂, R₃, and R₄, which may be the same or different, represent a hydrogen atom or a protecting group, comprising;

reacting a compound of formula (2)

wherein R₁ represents a hydrogen atom or a protecting group, with a compound having the formula (3)

wherein R₇ represents a hydrogen atom and R₂, R₃, and R₄, which are the same or different, represent a hydrogen atom or a protecting group.

2. A compound of the formula (1):

wherein R₇ represents a hydrogen atom and R₂, R₁, and R₄ represent a hydrogen atom or a protecting group.