Synthesis of medium and large phostams, phostones, and phostines

• Jiaxi Xu

Beilstein J. Org. Chem. 2023, 19, 687–699, doi:10.3762/bjoc.19.50

• refluxing acetonitrile for 6 h. It underwent a radical cyclization in refluxing benzene for 20 h to give rise to a nine-membered phostone thieno[2,3-d]pyrimidine-fused 2-hydroxy-1,2-oxaphosphonane 2-oxide 46 as a potential inhibitor after the deprotection of the benzyl group in the presence of DABCO in

• from 3-bromobut-3-en-1-yl ethenyl(phenyl)phosphinate and 2-bromophenylmethyl alk-1-enylphosphinates. Synthesis of thieno[2,3-d]pyrimidine-fused 2-hydroxy-1,2-oxaphosphonane 2-oxide from benzyl hydrogen allylphosphonate and 4-chloro-3-(chloromethyl)-2-(4-methylphenyl)benzo[b]thiophene. Synthesis of 3

C–C (alkynylation) vs C–O (ether) bond formation under Pd/C–Cu catalysis: synthesis and pharmacological evaluation of 4-alkynylthieno[2,3-d]pyrimidines

• Dhilli Rao Gorja,
• K. Shiva Kumar,
• K. Mukkanti and
• Manojit Pal

Beilstein J. Org. Chem. 2011, 7, 338–345, doi:10.3762/bjoc.7.44

• -alkynylthieno[2,3- d]pyrimidines were prepared via alkynylation of 4-chlorothieno[2,3-d]pyrimidines in good to excellent yields. Some of the compounds synthesized were tested for cytotoxic activity in vitro. Keywords: catalysis; C–C bond; copper; palladium; thieno[2,3-d]pyrimidine; Introduction Alkynyl

• highly express these kinases [6]. In continuation of our research program into new drug discovery, we became interested in the generation of a small-molecule library A (Figure 1) based on thieno[2,3-d]pyrimidine for in-house pharmacological evaluation. Accordingly, we recently reported the synthesis of 4

• -tetrahydro-5H-cyclohepta[4,5]thieno[2,3-d]pyrimidine (1d) was prepared from cycloheptanone and ethyl cyanoacetate following a similar procedure as shown in Scheme 2. Condensation of resulting amino ester, i.e., ethyl 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate (4) with formamide gave