In this regard, Fujian Institute of Microbiology (FIM) and Zhang et al. described the use of chiral lithium alkoxides obtained from amino alcohols (5, 6, 7, and 8) in combination with lithium amide bases in the BA reaction (Scheme 1a-b). The best stereoselectivity was achieved when employing the asymmetric compound 8, which provided a 16:1 d.r., and > 99 % ee in favor of the desired BDQ (3) stereoisomer. However, the reaction still suffered from low conversion to product; around 75 % of starting material remained unreacted. When combining 8 with a stronger lithium amide base such as lithium Nmethylpiperazide, conversion increased, while stereoselectivity decreased. Although the latter conditions provided a better overall yield for the 1,2-addition (83 % of 3+ent-3+4+ent-4), the BDQ (3) percentage in this mixture was only 45 %. Naicker et al. also reported an asymmetric approach for the BA reaction (Scheme 1a-b). In this case, the use of the chiral lithium amide base obtained from (R)-bis((R)-1phenylethyl)amine ( ) was studied. Despite some diastereoselectivity being achieved (9:1 d.r., syn:anti), conversion was extremely low (33 % by HPLC A %), and no enantioselectivity was observed. Herein, we report the use of chiral lithium amide bases derived from amino acids as affordable chiral transfer reagents to greatly improve the reactivity and stereoselectivity of the BA reaction currently being used to manufacture BDQ (3) for TB patients worldwide. In general, the transfer of chirality in reactions involving highly reactive intermediates, such as the lithiated intermediate 1a, offers even more challenge for the stereochemical control due to the fact that the background achiral reaction is often hard to slow down. This is the case with the BA reaction and why chiral transfer using chiral bases has been the preferred approach in this work. 18