title: Regioselective synthesis of 2-(bromomethyl)-5-aryl-thiophene derivatives via palladium (0) catalyzed suzuki cross-coupling reactions: as antithrombotic and haemolytically active molecules.
abstract: BACKGROUND
  It is seen that the regioselective functionalizations of halogenated heterocycles play an important role in the synthesis of several types of organic compounds. In this domain, the Suzuki-Miyaura reaction has emerged as a convenient way to build carbon-carbon bonds in synthesizing organic compounds. Some of the most important applications of these reactions can be seen in the synthesis of natural products, and in designing targeted pharmaceutical compounds. Herein, we present the regioselective synthesis of the novel series of 2-(bromomethyl)-5-aryl-thiophenes 3a-i, via Suzuki cross-coupling reactions of various aryl boronic acids with 2-bromo-5-(bromomethyl)thiophene (2).
  
  
  RESULTS
  The synthesized compounds were screened for their haemolytic and antithrombolytic activities. The novel compounds 3f, 3i showed highest 69.7, 33.6% haemolysis of blood cells, respectively. The antithrombolytic activity of the compounds was found to be within low to moderate against human blood clot. The compound 3i showed potent clot lysis (31.5%).
  
  
  CONCLUSIONS
  Considering these results, it is concluded that the synthesized compounds can be used as a promising source of therapeutic agents.
authors: Department of Chemistry, Government College University, Faisalabad, 38000 Pakistan.
authors: Komal
authors: K
authors: Rizwan
authors: Department of Chemistry, Government College University, Faisalabad, 38000 Pakistan.
authors: Muhammad
authors: M
authors: Zubair
authors: Department of Chemistry, Government College University, Faisalabad, 38000 Pakistan.
authors: Nasir
authors: N
authors: Rasool
authors: Department of Chemistry, Government College University, Faisalabad, 38000 Pakistan.
authors: Shaukat
authors: S
authors: Ali
authors: Department of Chemistry, Government College University, Faisalabad, 38000 Pakistan.
authors: Ameer Fawad
authors: AF
authors: Zahoor
authors: Sustainable Energy Technologies (SET) Center, College of Engineering, King Saud University, PO-Box - 800, Riyadh, 11421 Saudi Arabia.
authors: Usman Ali
authors: UA
authors: Rana
authors: Sustainable Energy Technologies (SET) Center, College of Engineering, King Saud University, PO-Box - 800, Riyadh, 11421 Saudi Arabia.
authors: Salah Ud-Din
authors: SU
authors: Khan
authors: Department of Chemistry and Biochemistry, University of Agriculture, Faisalabad, 38040 Pakistan.
authors: Muhammad
authors: M
authors: Shahid
authors: The Patent Office, Karachi, Pakistan.
authors: Muhammad
authors: M
authors: Zia-Ul-Haq
authors: Department of Crop Science, Faculty of Agriculture, 43400 UPM Serdang, Selangor Malaysia.
authors: Hawa Ze
authors: HZ
authors: Jaafar
keywords: Antithrombotic; Aryl boronic acid; Cytotoxicity; Haemolytic; Heterocycles; Palladium; Suzuki cross-coupling reactions; Thiophene