Hubei YYD Industrial Co., Ltd.

Aspartame Synthesis Method

Jun 28, 2022


Aspartame, APM, also known as Aspartame or saccharide (international code of food additives: E951), chemical name Aspartame phenylalanine methyl ester, is a non-carbohydrate artificial sweetener.  Aspartame was successfully synthesized and patented in 1965, and the patent expired in 1992.  It is a white crystalline powder at room temperature.  Asba is high in sweetness, pure in sweetness, without caries, low in heat, low in hygroscopicity and no sticky phenomenon. It is mainly used in drinks, vitamin lozenges or chewing gum instead of sugar.  Many diabetics and dieters use aspartame as a sugar substitute.  But heat causes it to break down and lose its sweetness, making it unsuitable for cooking and hot drinks.


Aspartame is about 200 times sweeter than sugar and has fewer calories than table sugar. One gram of aspartame has about 4 calories. The amount of aspartame needed to taste sweet is so small that the calories are negligible, and it is widely used as an alternative to table sugar. Aspartame has a different taste from regular table sugar. The sweetness of aspartame is delayed and lasts longer than that of sugar, but some consumers find it unacceptable, so some consumers do not like using substitute sugar. When potassium acetosulfonate is mixed with aspartame, the resulting taste may be more like sugar.


The synthetic methods

Aspartame can be produced by esterification of L-phenylalanine with methanol and then condensation and amidation of L-aspartic acid. Some synthetic methods are patent-protected, and many of the details are secret.


There are two synthetic methods for commercial use.


The addition of two carboxyl aspartic acid to an anhydride, a compound protected by an amino group, will prevent further reactions. Thus, phenylalanine is methylated and bound to the "N" -protected aspartic anhydride, removing the blocking group from the aspartic acid by acid hydrolysis. The downside of this technique is the production of a byproduct - the bitter β- type (when aspartic acid is mislinked to form the carboxyl phenylalanine). Catalysis with Thermoproteolyticus enzyme will increase the yield. This method has not been used for commercial purposes. Unmodified aspartic acid was used, but the yield was low.


The second is the methylation method, direct production of aspartic acid phenylalanine. But not for industrial use.



use

More than 90 countries around the world approve the use of aspartame as a food additive. The U.S. Food and Drug Administration says it's a safe sweetener. The use of aspartame was controversial in the early days. Some studies cannot rule out the possibility that aspartame could cause brain tumors, brain damage and lymphatic cancer. That's why the FOOD and Drug Administration didn't approve the use of aspartame in food for years. These findings were controversial during the approval process, as they had clear conflicts of interest with the companies that make aspartame. Beginning in 1983, the FDA gradually relaxed restrictions on the use of aspartame until all restrictions were lifted in 1996.


Japan has approved aspartame as a food additive since 1983. Because the chemical structure contains the amino acid phenylalanine, people with phenylketonuria cannot metabolize this amino acid, and people with phenylketonuria must avoid aspartame.


Aspartame sells more than $1 billion a year in thousands of products, including vitamins and calcium tablets for children. Coca-Cola's Diet Coke and the newly launched Coca-Cola Zero use aspartame as a sweetener, and some restaurants offer aspartame as a choice.


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