Organic compounds -- part of the class 532-570 series – Organic compounds – Rare earth containing
Patent
1996-07-16
1998-02-03
Kight, John
Organic compounds -- part of the class 532-570 series
Organic compounds
Rare earth containing
568 4, 564 8, 424 165, 424 9364, C07F 500, C07F 502, A61K 4900, A61K 5100
Patent
active
057145911
ABSTRACT:
The present invention provides a gadolinium-DTPA complex containing a carborane unit having structural formula (1) given below and an intermediate thereof, i.e., carborane-containing DTPA derivative represented by formula (2) given below. ##STR1## The present invention also provides a method of synthesizing the compound (1), which comprises reacting an ester derivative of DTPA with a carborane derivative in the presence of a palladium catalyst, deesterifying by treatment with an acid, reacting with gadolinium trichloride hexahydrate, and treating with an alkali to give the desired compound (1).
REFERENCES:
patent: 4959356 (1990-09-01), Miura et al.
patent: 5286853 (1994-02-01), Spielvogel et al.
Progress in Neutron Capture Therapy for Cancer, pp. 231-233, 1992, A.D. Whittaker, et al., "Synthesis of .sup.10 B-and .sup.157 Gd-Labelled DNA Ligands for Neutron Capture Therapy".
Phys. Med. Biol., 1992, vol. 37, No. 1, pp. 155-162, Tetsuo Matsumoto, "Transport Calculations of Depth-Dose Distributions for Gadolinium Neutron Capture Therapy".
Tetrahedron Letters, vol. 37, No. 4, pp. 539-542, Jan. 22, 1996, Hisao Nemoto, et al., "A New Synthetic Method of All Carboxylate-Free DTPA Derivatives and its Application to the Synthesis of Gd-Carborane Complex".
1995 International Chemical Congress, Dec. 17-22, 1995, abstract of the presentation by Dr. Jianping Cai, et al., "Synthesis of All Carboxylate-Free DTPA Derivatives Via Palladium Catalyzed Carbon-Carbon Bond Formation Reaction".
Database WPI, Derwent Publications, AN 96-175722, JP-A-8 053 475, Feb. 27, 1996.
Nemoto Hisao
Yamamoto Yoshinori
Kelley Lara C.
Kight John
President of Tohoku University
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