This review presents the synthesis of organoaluminum steroids (OAS) using catalytic cycloalumination of vinylcholestane and/or allylcholestane derivatives with Et 3 Al catalyzed by Cp 2 ZrCl 2 which gives aluminacyclopentanes in a yield of about 90 %. Biological activity of synthesized organoaluminum steroids was determined with an aid of PASS program. Organoaluminum steroids showed antiprotozoal, antihypercholesterolemic, and antieczematic activity with a certainty from 78 to 92 %. Scheme 1: Reagents and conditions: i. PCC (pyridiniumchlorochromate), Al 2 O 3 , C 6 H 6 (81 %); ii. Ph 3 P=CH 2 , DMSO, C 6 H 6 (88 %); iii. Cl 3 CCOCl, Zn (64 %); iv. Zn, AcOH; v. Ph 3 P=CH 2 , DMSO, C 6 H 6 (74 %); vi. Cp 2 ZrCl 2 , Et 3 Al; vii. CuSO 4 /SiO 2 (72 %) Scheme 2: Synthesis of compound 15. Reagents and conditions: i. PCC (pyridiniumchlorochromate)-Al 2 O 3 , C 6 H 6 (81 %); ii. Ph 3 P=CHCH 2 SiMe 3 , THF (85 %); iii. BF 3 /AcOH (89 %); iv. Et 3 Al (3 eq.), Cp 2 ZrCl 2 (10 %)