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BioBlocks

BioBlocks Bulletin
Vol. 10 August 2009
Welcome to the BioBlocks Bulletin

The BioBlocks Bulletin brings you recent research on key classes of building blocks. In this issue we describe applications with products derived from 2-carboxyquinazolines. Members of this family have been used as blood clotting pathway modulators, anti-tumor agents and as treatment for cardiovascular diseases. If you are interested in a related compound, please contact us for inclusion in the growing set of analogs.

In this issue we present 15 2-carboxyquinazolines

The schemes below describe three applications of this product class to medicinal chemistry programs. At BioBlocks, we believe that providing SAR options is an important goal and have initiated a program to generate a range of these versatile compounds in research quantities.

Our catalog currently contains 15 items from this class. Shown below is a list of available 2-carboxyquinazolines starting materials, highlighting the range of substitutions available for SAR in your project.

Please scroll down to the bottom of the newsletter to view the references. To order products, shop at www.bioblocks.com, call (+1) 858 558-5900 or email sales@bioblocks.com.

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Our results-based lead optimization services focus on your project goals. Learn how we can be a cost efficient, innovative resource for your medicinal chemistry needs.
Application Update
Scheme
  Mjalli, Adnan M. M., et al., WO2005014533.
Scheme
  Cai, Sui Xiong, et al., WO2005003100.
Scheme
  Nagarathnam, Dhanapalan, et al., WO2002076976.
Featured Products
QZ001

QZ001
4-Chloro-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $245.00
QZ002

QZ002
Quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $325.00
QZ003

QZ003
Quinazoline-2-carboxylic acid
Price: 1g = $520.00
QZ004

QZ004
4-Chloro-6-methyl-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $250.00
QZ005

QZ005
6-Methyl-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $400.00
QZ006-1

QZ006-1
6-Methyl-quinazoline-2-carboxylic acid
Price: 1g = $585.00
QZ008

QZ008
6-Bromo-4-chloro-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $250.00
QZ009

QZ009
4,6-Dichloro-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $285.00
QZ010

QZ010
4-Chloro-7-fluoro-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $260.00
QZ011

QZ011
4-Chloro-7-trifluoromethyl-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $245.00
QZ013

QZ013
4-Chloro-6-methoxy-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $250.00
QZ016

QZ016
4,7-Dichloro-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $240.00
QZ017

QZ017
4-Chloro-6,7-dimethoxy-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $245.00
QZ018

QZ018
4-Chloro-7-methoxy-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $300.00
QZ019

QZ019
7-Bromo-4-chloro-quinazoline-2-carboxylic acid ethyl ester
Price: 1g = $250.00
Literature References
1. Mjalli, Adnan M. M.; Andrews, Robert C.; Guo, Xiao-Chuan; Christen, Daniel Peter; Gohimmukkula, Devi Reddy; Huang, Guoxiang; Rothlein, Robert; Tyagi, Sameer; Yaramasu, Tripura; Behme, Christopher
Preparation of aryl and heteroaryl amino acid derivatives as antagonists of factor IX and/or factor XI.
WO2005014533

In this patent from Transtech Pharma, scientists present a series of modulators of the intrinsic clotting pathway. Synthetic routes to transform BioBlocks QZ013 from 4-chloro-6-methoxy-quinazoline-2-carboxylic acid ethyl ester to the 4-ethylsulfanyl-6-hydroxy-quinazoline-2-carboxylic acid are described. Further derivitization via standard HBTU amide coupling conditions followed by copper mediated o-arylation led to a small set of the claimed modulators.
2. Cai, Sui Xiong; Sirisoma, Nilantha Sudath; Pervin, Azra; Drewe, John A.; Kasibhatla, Shailaja; Jaing, Songchun; Zhang, Hong; Pleiman, Chris; Baichwal, Vijay; Manfredi, John; Bhoite, Leena
Preparation of 4-arylaminoquinazolines and analogs as activators of caspases and inducers of apoptosis.
WO2005003100

Scientists from Myriad Genetics and Cytovia disclose the use of 4-arylamino-quinazolines and analogs as caspase activators and inducers of apoptosis. There is evidence that cancer cells, while containing caspases, lack parts of the molecular machinery that activates the caspase cascade. 4-anilino-quinazolines are described as potential chemotherapeutic drugs which trigger apoptosis by reactivating the cascade. The described compounds were readily accessed by displacement of the chlorine in QZ001 with anilines under acidic conditions at elevated temperatures.
3. Nagarathnam, Dhanapalan; Asgari, Davoud; Shao, Jianxing; Liu, Xiao-Gao; Khire, Uday; Wang, Chunguang; Hart, Barry; Boyer, Stephen; Weber, Olaf; Lynch, Mark; Bankston, Donald.
Preparation of (indazol-5-ylamino)quinazolines as Rho-kinase inhibitors.
WO2002076976

Bayer scientists describes the synthesis and derivitization of quinazolines to be used as Rho-kinase inhibitors. Such compounds display tumor growth inhibition and promising treatment for cardiovascular disease. Synthetic procedures to transform the key bifunctional intermediate, BioBlocks QZ001 from the 2-carboethoxy-4-chloro- starting material to the 2-carboethoxy-4-aminoindazole are described and follow similarly to reference 2 above. A series of amides is then derived from the 2-carboethoxy-4-aminoindazole via trimethylaluminum mediated amide formation.



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